Search Result
Results for "
competitive inhibitor
" in MedChemExpress (MCE) Product Catalog:
1626
Inhibitors & Agonists
14
Biochemical Assay Reagents
95
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-117043
-
|
|
Deubiquitinase
SARS-CoV
|
Infection
|
|
GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome .
|
-
-
- HY-11007
-
GNF-2
2 Publications Verification
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
-
- HY-126388
-
-
-
- HY-149527
-
-
-
- HY-134246
-
|
5'-dTuMP
|
Others
|
Others
|
|
7-CH-5'-dAMP (5'-dTuMP) is an adenylate derivative that acts as a potential substrate, competitive inhibitor, or modulator of enzymes that interact with 2-deoxyadenosine-5-monophosphate .
|
-
-
- HY-168079
-
|
|
GSK-3
Tau Protein
|
Neurological Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3β inhibitor (IC50=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitory activities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .
|
-
-
- HY-134280
-
|
Nicotinamide 8-Br-hypoxanthine dinucleotide
|
Others
|
Others
|
|
8-Br-NHD+ (Nicotinamide 8-Br-hypoxanthine dinucleotide) is a derivative of NAD+ (nicotinamide adenine dinucleotide) that acts as a potential substrate, competitive inhibitor or modulator of enzymes that interact with β-NAD+. 8-Br-NHD+ can be used to synthesize a cyclic ADP nucleotide (cADPR) analog .
|
-
-
- HY-116621
-
|
|
DNA-PK
|
Cancer
|
|
NU-7163 is an ATP-competitive DNA-PK inhibitor (IC50=0.19 μM; Ki=24 nM). NU-7163 enhances the cytotoxicity of ionizing radiation against the HeLa human tumor cell line in vitro .
|
-
-
- HY-123171
-
|
|
Others
|
Metabolic Disease
|
|
ASP8497 is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor that reduces blood glucose levels and increases plasma active GLP-1 and insulin levels without causing hypoglycemia in fasted normal mice. ASP8497 can be utilized for antihyperglycemic research .
|
-
-
- HY-129412
-
|
|
Renin
|
Cardiovascular Disease
|
|
A-74273 is an orally active peptide renin inhibitor (IC50=3.1 nM). A-74273 competitively binds to the active site of renin, preventing angiotensinogen from being converted to ANG-I, thereby reducing the level of angiotensin II. A-74273 can be used in the study of diseases such as hypertension .
|
-
-
- HY-114858
-
|
|
Casein Kinase
|
Cancer
|
|
Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1 .
|
-
-
- HY-15295
-
|
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease .
|
-
-
- HY-100007A
-
|
TAK-438 hydrochloride
|
Proton Pump
Bacterial
|
Infection
Endocrinology
|
|
Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan hydrochloride is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride can be used for eradication of Helicobacter pylori .
|
-
-
- HY-100007
-
|
TAK-438 free base
|
Proton Pump
Bacterial
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
|
-
-
- HY-100007R
-
|
TAK-438 (Standard)
|
Proton Pump
Bacterial
|
Endocrinology
|
|
Vonoprazan (Standard) is the analytical standard of Vonoprazan. This product is intended for research and analytical applications. Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
|
-
-
- HY-161507
-
|
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Metabolic Disease
|
|
hCAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. hCAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC50 = 21.35 ± 0.39 nM (hCA I); 7.12 ± 0.12 nM (hCA II)). hCAI/II-IN-8 inhibits AChE and BChE as well(IC50 = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). . .
|
-
-
- HY-149404
-
|
|
Reactive Oxygen Species
Tyrosinase
|
Others
|
|
Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) is a potent, non-competitive tyrosinase inhibitor with an IC50 value of 49.33 ± 2.64 µM and Ki value of 31.25 ± 0.25 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) have the highest radical scavenging activity to reduce the production of reactive oxygen species (ROS) with an IC50 value of 25.39 ± 0.77 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) can be used for anti-browning substances in the food and agricultural sectors .
|
-
-
- HY-B1413
-
-
-
- HY-131408
-
|
|
Others
|
Others
|
|
L-Allooctopine is a competitive inhibitor of D-octopine .
|
-
-
- HY-N3090
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
|
-
-
- HY-147167
-
-
-
- HY-22385
-
-
-
- HY-135072
-
|
|
Others
|
Infection
|
|
N,N',N''-Triacetylchitotriose is a competitive inhibitor of lysozyme .
|
-
-
- HY-109079A
-
|
DWP14012 hydrochloride; Fexuprazan hydrochloride
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
-
- HY-109079
-
|
DWP14012; Fexuprazan
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
-
- HY-19593
-
|
|
Fungal
Antibiotic
|
Infection
|
|
Nikkomycin Z, a nucleoside-peptide, is a selective competitive chitin synthesis inhibitor. Nikkomycin Z has antifungal effects and acts as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine .
|
-
-
- HY-115939
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-2 (compound 8g) is a non-competitive urease inhibitor with an IC50 of 0.94 μM and a Ki of 1.6 μM. Urease-IN-2 inhibits the Jack bean urease (JBU) in a non-competitive manner .
|
-
-
- HY-50948
-
-
-
- HY-17502
-
-
-
- HY-N2194
-
|
5-Geranoxypsoralen; Bergamotine; Bergaptin
|
Cytochrome P450
|
Cancer
|
|
Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
|
-
-
- HY-W013673
-
-
-
- HY-W013744
-
|
|
Others
|
Others
|
|
S-Octylglutathione is a competitive glutathione S-transferase (GST) inhibitor .
|
-
-
- HY-126306
-
-
-
- HY-101631
-
-
-
- HY-126055
-
|
|
Others
|
Others
|
|
Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
-
- HY-126055A
-
|
|
Others
|
Others
|
|
Hadacidin sodium is a competitive inhibitor of adenylate synthase. Hadacidin sodium binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin sodium can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
-
- HY-B0140
-
-
-
- HY-14806
-
|
MP-513
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
|
-
-
- HY-B1239
-
-
-
- HY-13646A
-
|
HM30181 mesylate; HM30181A mesylate
|
P-glycoprotein
|
Cancer
|
|
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
|
-
-
- HY-22385A
-
-
-
- HY-W015876
-
|
(+)-Leucinol
|
Aminopeptidase
|
Others
|
|
L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM .
|
-
-
- HY-116290
-
|
Squalestatin S1
|
Others
|
Others
|
|
Zaragozic acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
|
-
-
- HY-119409
-
-
-
- HY-E70252
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
1-Pyrenebutanoyl-CoA is a type of coenzyme A that can non-competitively inhibit (Ki = 2 μM) phosphorylating (ADP-stimulated) respiration in rat liver mitochondria, and competitively inhibit (Ki = 2.1 μM and 15 μM) carnitine palmitoyl-CoA transferase and octanoyl-CoA transferase .
|
-
-
- HY-Y0504
-
|
Hegzadesil; Trimethylamine hydrochloric acid; Trimethylamine monohydrochloride
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
|
-
-
- HY-10450S
-
|
BMS-512148-d5
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin-d5 is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor[1].
|
-
-
- HY-12054A
-
-
-
- HY-P1292
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
-
- HY-103351
-
-
- HY-11092
-
-
- HY-12471
-
VLX1570
2 Publications Verification
|
Deubiquitinase
|
Cancer
|
|
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
|
-
- HY-16461
-
|
(-)-Solenopsin A
|
Akt
|
Cardiovascular Disease
|
|
Solenopsin ((-)-Solenopsin A) is an ATP-competitive AKT inhibitor with IC50 value of 10 μM .
|
-
- HY-W010510
-
-
- HY-122641A
-
-
- HY-122641C
-
-
- HY-135404
-
-
- HY-50949
-
-
- HY-115743
-
|
|
MAP3K
|
Cancer
|
|
TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
|
-
- HY-15269
-
|
|
mTOR
PI3K
|
Cancer
|
|
PP30, a TORKinib, is a potent, selective, and ATP-competitive inhibitor of mTOR with an IC50 of 80 nM.
|
-
- HY-112465
-
|
|
PKA
|
Cancer
|
|
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor .
|
-
- HY-W000932
-
|
|
Bacterial
|
Infection
|
|
Butylboronic acid is a competitive soybean urease inhibitor with an IC50 of 2.9 mM and a Ki of 1.5 mM .
|
-
- HY-116290A
-
|
Squalestatin S1 trisodium
|
Others
|
Others
|
|
Zaragozic acid A trisodium is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
|
-
- HY-134382
-
|
7-Deaza-2'-deoxyadenosine-5'-O-diphosphate
|
Others
|
Others
|
|
7-CH-dADP is a competitive inhibitor or regulator of enzymes that interact with dADP .
|
-
- HY-B1239A
-
-
- HY-112860
-
-
- HY-P1292A
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-118177
-
-
- HY-163974
-
-
- HY-162059
-
|
|
Pim
Apoptosis
Caspase
|
Cancer
|
|
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
|
-
- HY-12382
-
|
|
Mps1
|
Cancer
|
|
NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
|
-
- HY-B1258
-
|
Aminomethylbenzoic acid; α-Amino-p-toluic acid
|
Amino Acid Derivatives
|
Cancer
|
|
4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
|
-
- HY-16194
-
|
BAY o 1248
|
Others
|
Metabolic Disease
|
|
Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
|
-
- HY-101769
-
|
|
Dipeptidyl Peptidase
|
Cancer
|
|
UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
|
-
- HY-122641B
-
-
- HY-20558
-
-
- HY-145678
-
|
|
Others
|
Metabolic Disease
|
|
α-HNJNAc is a potent, competitive hexosaminidases inhibitor without interfering with other glycosidases .
|
-
- HY-P4543
-
-
- HY-148394
-
|
|
Others
|
Infection
Cancer
|
|
UCK2 Inhibitor-1 (Compound 20874830-2) is a non-competitive UCK2 inhibitor with an IC50 of 4.7 µM .
|
-
- HY-112392
-
|
|
GSK-3
|
Cancer
|
|
GSK-3 Inhibitor XIII is a potent and ATP-competitive GSK-3 inhibitor with a Ki of 24 nM .
|
-
- HY-P1315
-
|
Glycylglycyl-L-tyrosyl-L-arginine
|
Cathepsin
|
Others
|
|
Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2 .
|
-
- HY-12660
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
|
-
- HY-16902
-
|
|
Syk
|
Inflammation/Immunology
|
|
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
|
-
- HY-110399
-
-
- HY-101334
-
|
|
GlyT
|
Neurological Disease
|
|
MPDC is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
|
-
- HY-135405
-
-
- HY-113894
-
|
|
Aurora Kinase
|
Cancer
|
|
Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor .
|
-
- HY-N3906
-
-
- HY-122439
-
-
- HY-135436
-
|
|
IGF-1R
|
Cancer
|
|
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM .
|
-
- HY-101334A
-
|
|
GlyT
|
Neurological Disease
|
|
MPDC hydrochloride is a potent and competitive inhibitor of the Na +-dependent high-affinity glutamate transporter in forebrain synaptosomes .
|
-
- HY-P10657
-
-
- HY-124163
-
-
- HY-13452
-
|
ML282
|
Ras
|
Inflammation/Immunology
|
|
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
|
-
- HY-112333
-
-
- HY-149775
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-10 (Conjugate 4) is a competitive Urease inhibitor, with an IC50 of 3.59±0.07 μM and a Ki of 7.45 μM. Urease-IN-10 is a conjugate consisting of Diclofenac (HY-15036) and Sulfanilamide (HY-B0242). Diclofenac-sulfanilamide inhibits the Jack bean urease(JBU) in a competitive manner .
|
-
- HY-112914
-
|
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-1 (Compound C-4) is an ATP-Competitive mTOR inhibitor which can suppress cells proliferation and inducing autophagy .
|
-
- HY-117769
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
|
-
- HY-114511
-
|
|
Factor VIIa
|
Cardiovascular Disease
|
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
|
-
- HY-16982
-
|
(-)-Cercosporamide
|
Fungal
MNK
PKC
|
Infection
Cancer
|
|
Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-149524
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC50: 5.38 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-149525
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC50: 4.07 μM) of sirtuin SIRT5 with anticancer potential .
|
-
- HY-119582
-
|
|
Others
|
Inflammation/Immunology
|
|
Safironil is an antifibrotic compound. Safironil is a competitive inhibitor of collagen protein synthesis. Safironil reduces liver fibrogenesis by inhibiting HSC activation .
|
-
- HY-149888
-
-
- HY-155600
-
|
β,γ-Methylene-GTP sodium
|
Others
|
Others
|
|
5′-Guanylyl methylenediphosphonate (sodium) is a GTP analogue and a specific, competitive inhibitor of the GTP reaction in protein synthesis .
|
-
- HY-10992
-
-
- HY-15512A
-
|
OTS167 hydrochloride
|
MELK
|
Cancer
|
|
OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.
|
-
- HY-N1201
-
-
- HY-104009A
-
|
|
Histone Methyltransferase
|
Others
|
|
GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM .
|
-
- HY-13503
-
-
- HY-B0183A
-
|
|
Casein Kinase
|
Cancer
|
|
Ellagic acid hydrate is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM .
|
-
- HY-14715
-
-
- HY-16015
-
|
ABC294640
|
SphK
|
Cancer
|
|
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
|
-
- HY-15512
-
|
OTS167
|
MELK
|
Cancer
|
|
OTSSP167 (OTS167) is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.
|
-
- HY-110331
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM .
|
-
- HY-10992A
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
|
-
- HY-N11521
-
|
|
Tyrosinase
|
Cancer
|
|
7-Methoxy obtusifolin (Compound 4) is a competitive tyrosinase inhibitor with an IC50 of 7.0 μM .
|
-
- HY-N12427
-
|
|
Tyrosinase
|
Cancer
|
|
Litchinol B (compound 2) is a non-competitive tyrosinase inhibitor with an inhibition constant of 5.70 μM .
|
-
- HY-16015A
-
|
ABC294640 hydrochloride
|
SphK
|
Cancer
|
|
Opaganib (ABC294640) hydrochloride is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
|
-
- HY-159628A
-
-
- HY-14806R
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (Standard) is the analytical standard of Teneligliptin. This product is intended for research and analytical applications. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
|
-
- HY-14806S1
-
|
MP-513-d4
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
- HY-112355
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively .
|
-
- HY-15247
-
|
AZD2014
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
|
-
- HY-13966
-
|
2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose
|
Hexokinase
HSV
Apoptosis
|
Cancer
|
|
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
|
-
- HY-101053
-
|
Src Kinase inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-15656S
-
-
- HY-121787
-
|
OLC20
|
Others
|
Others
|
|
OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
|
-
- HY-14731
-
|
|
ATM/ATR
|
Cancer
|
|
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
|
-
- HY-17353
-
|
|
Telomerase
Apoptosis
|
Cancer
|
|
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
|
-
- HY-15465
-
|
|
CaMK
Autophagy
|
Cancer
|
|
KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
|
-
- HY-77195
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.
|
-
- HY-15465A
-
|
|
CaMK
Autophagy
|
Cancer
|
|
KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
|
-
- HY-B0183
-
-
- HY-50703
-
MK-2461
1 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
|
-
- HY-13447A
-
-
- HY-136347
-
-
- HY-W013386
-
-
- HY-P3786
-
|
|
PKA
PKC
|
Cancer
|
|
H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
|
-
- HY-13447
-
-
- HY-154828
-
|
3′,5′-UDP
|
DNA/RNA Synthesis
|
Others
|
|
Uridine 3′,5′-diphosphate (3′,5′-UDP; Compound pUp) is a competitive RNase inhibitor .
|
-
- HY-129298
-
|
|
Aminopeptidase
|
Others
|
|
Amastatin is A slow, tightly bound, competitive inhibitor of aminopeptidase (AP) with an IC50 of 0.54 μg/mL for AP-A .
|
-
- HY-104050
-
M-31850
1 Publications Verification
|
Others
|
Metabolic Disease
|
|
M-31850 is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor with IC50s of 6.0 µM and 3.1 µM for human HexA and human HexB, respectively. M-31850 also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM .
|
-
- HY-B0140R
-
|
|
Phosphodiesterase (PDE)
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
Aminophylline (Standard) is the analytical standard of Aminophylline. This product is intended for research and analytical applications. Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research .
|
-
- HY-13806
-
XL388
3 Publications Verification
|
mTOR
Autophagy
|
Cancer
|
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
- HY-10366
-
BI-78D3
1 Publications Verification
|
JNK
|
Metabolic Disease
Cancer
|
|
BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM).
|
-
- HY-115748
-
-
- HY-N3394
-
|
|
Others
|
Infection
|
|
Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase .
|
-
- HY-112487
-
|
|
Acyltransferase
|
Endocrinology
|
|
Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT). Sandoz 58-035 effectively inhibits (>98%) hormonally stimulated cholesterol esterification in cells .
|
-
- HY-50877
-
|
GSK461364A
|
Polo-like Kinase (PLK)
|
Cancer
|
|
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
|
-
- HY-14394
-
|
NSC 231634; Casein Kinase II inhibitor I
|
Casein Kinase
|
Cancer
|
|
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
|
-
- HY-13949
-
|
SRPK inhibitor
|
SRPK
Virus Protease
|
Cancer
|
|
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
|
-
- HY-B0165
-
-
- HY-13823
-
-
- HY-112945
-
|
|
Others
|
Metabolic Disease
|
|
MLS0315771 is a potent and biologically active competitive phosphomannose isomerase (MPI) inhibitor, with an IC50 ~1 μM and a Ki of 1.4 μM.
|
-
- HY-126253
-
-
- HY-136344
-
|
|
Drug Metabolite
|
Others
|
|
Simvastatin Acyl-β-D-glucuronide is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
|
-
- HY-W042648
-
|
|
Casein Kinase
|
Others
|
|
4,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor .
|
-
- HY-20696
-
|
Tryptoline
|
5-HT Receptor
|
Metabolic Disease
|
|
Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM .
|
-
- HY-78036
-
|
Citronic acid; Methylfumaric acid
|
Endogenous Metabolite
|
Others
|
|
Mesaconic acid is an active product that can be extracted from Saxifraga stolonifera. Mesaconic acid is used as a fire retardant and is a competitive inhibitor of fumarate reduction .
|
-
- HY-W278777
-
|
|
Others
|
Others
|
|
Monohexyl phthalate is a competitive inhibitor towards UGT1A9, with an IC50 of 12.46 μM and a Ki of 7.47 μM .
|
-
- HY-131816
-
|
|
Others
|
Others
|
|
5'-dUMPS is a competitive inhibitor or regulator of enzymes that interacts with 2′-deoxypyrimidine-5′-monophosphate .
|
-
- HY-162711
-
|
|
Others
|
Cancer
|
|
Methylbiocin is an ATP competitive inhibitor for human CMG helicase with an IC50 of 59 µM. Methylbiocin exhibits potential in cancer research .
|
-
- HY-117672
-
|
|
Phosphatase
|
Others
|
|
L-671776 can be isolated from a fungal strain (ATCC 20928B), is a non-competitive inhibitor of IMPase .
|
-
- HY-12042A
-
|
AS703026 hydrochloride; MSC1936369B hydrochloride
|
MEK
|
Cancer
|
|
Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
|
-
- HY-10005
-
|
HMR-1275; Alvocidib; L86-8275
|
CDK
Autophagy
HIV
Apoptosis
|
Cancer
|
|
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-70035
-
|
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- HY-15248
-
|
|
mTOR
Autophagy
|
Cancer
|
|
GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
|
-
- HY-112080
-
|
|
Histone Methyltransferase
|
Cancer
|
|
BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM .
|
-
- HY-101578
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
|
-
- HY-14761
-
|
AS 602801
|
JNK
|
Cancer
|
|
Bentamapimod (AS 602801) is an ATP-competitive JNK inhibitor with IC50 of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively.
|
-
- HY-15646
-
-
- HY-13805
-
|
AGL 1879
|
Src
|
Cancer
|
|
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
|
-
- HY-I0020
-
|
(-)-Narwedine; Narwedin
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
|
-
- HY-13298
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM .
|
-
- HY-B1542A
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Benactyzine hydrochloride is a competitive BChE inhibitor with a Ki of 0.01 mM. Benactyzine hydrochloride is an anticholinergic drug. Benactyzine hydrochloride has the potential for organophosphate poisoning research .
|
-
- HY-19677
-
|
Ro 32-3555
|
MMP
|
Cancer
|
|
Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.
|
-
- HY-B0242S1
-
|
Sulphanilamide-d4
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
|
-
- HY-125643
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Pitavastatin lactone is a major metabolite of Pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes .
|
-
- HY-33914
-
-
- HY-136345
-
|
|
Drug Metabolite
|
Others
|
|
(Rac)-3′-Hydroxy simvastatin is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
|
-
- HY-122933
-
-
- HY-120279A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM) .
|
-
- HY-105375
-
|
|
Cytochrome P450
|
Cancer
|
|
FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research .
|
-
- HY-160124
-
|
|
FGFR
|
Cancer
|
|
Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor .
|
-
- HY-127178
-
|
|
Phosphatase
|
Cancer
|
|
ML120 analog 1 (compound 1) is a competitive inhibitor with a Ki of 0.69 μM for Hematopoietic protein tyrosine phosphatase (HePTP) .
|
-
- HY-N2087
-
|
|
Others
|
Metabolic Disease
|
|
Ligupurpuroside A is an active product that can be extracted from Ligustrum robustum. Ligupurpuroside A acts as a natural inhibitor of lipase in a competitive manner .
|
-
- HY-138165
-
|
|
Others
|
Others
|
|
Ac-Phe-NH2 is a non-competitive inhibitor of polyubiquitin chain elongation at Ki value of 8 mM by destabilizing the active trimer .
|
-
- HY-14486
-
|
PRT060128 potassium
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Elinogrel (PRT060128) potassium is a reversible, competitive and orally active P2Y12 antagonist. Elinogrel potassium inhibits thrombosis .
|
-
- HY-161680
-
|
|
Others
|
Cancer
|
|
Pyruvate Carboxylase-IN-4 (Compd 8V) is a potent and competitive Pyruvate Carboxylase inhibitor with an IC50 of 4.3 μM .
|
-
- HY-131812
-
|
2'-Deoxyadenosine 5'-O-thiophosphate
|
Others
|
Others
|
|
5'-dAMPS is an analogue of 5'-dAMP and thus a potential substrate, competitive inhibitor or regulator of enzymes that interact with dAMP .
|
-
- HY-131810
-
|
|
Others
|
Others
|
|
5'-AMPS is an analogue of 5'-AMP and a substrate and competitive inhibitor or regulator of enzymes that interact with 5'-AMP .
|
-
- HY-164371
-
|
|
Androgen Receptor
|
Cancer
|
|
(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
|
-
- HY-B1542
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Benactyzine is a competitive BChE inhibitor with a Ki of 0.01 mM. Benactyzine is an anticholinergic drug. Benactyzine has the potential for organophosphate poisoning research .
|
-
- HY-115748A
-
-
- HY-153176
-
|
|
Ras
|
Cancer
|
|
PAT-IN-1 is a protein acyl transferases (PAT) inhibitor. PAT-IN-1 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 13) .
|
-
- HY-153177
-
|
|
Ras
|
Cancer
|
|
PAT-IN-2 is a protein acyl transferases (PAT) inhibitor. PAT-IN-2 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 25) .
|
-
- HY-162149
-
|
|
Bacterial
|
Infection
|
|
Urease-IN-12 (compound 5e) is a competitive urease inhibitor (IC50: 0.35 μM) with the potential to inhibit gastritis and peptic ulcer caused by Helicobacter pylori .
|
-
- HY-152214
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
|
-
- HY-147879
-
-
- HY-12042
-
|
AS703026; MSC1936369B
|
MEK
|
Cancer
|
|
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
|
-
- HY-15251
-
-
- HY-13820
-
|
|
PERK
Autophagy
Apoptosis
|
Cancer
|
|
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
|
-
- HY-12465
-
|
Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII
|
Notch
γ-secretase
Apoptosis
|
Cancer
|
|
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch .
|
-
- HY-12524
-
Bikinin
1 Publications Verification
Abrasin
|
GSK-3
|
Others
|
|
Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
|
-
- HY-101503
-
|
|
FABP
|
Metabolic Disease
|
|
HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- HY-114349
-
-
- HY-W020215
-
-
- HY-114503
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-10243
-
|
MK-7009
|
HCV
HCV Protease
|
Infection
|
|
Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
|
-
- HY-132907
-
-
- HY-W092533
-
|
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes .
|
-
- HY-129450
-
|
|
Others
|
Others
|
|
Ethyl-L-NIO hydrochloride is a potent and competitive human dimethylarginine dimethylaminohydrolase 1 (hDDAH-1) inhibitor with an IC50 of 70 μM and a Ki of 32 μM .
|
-
- HY-124230
-
|
|
15-PGDH
|
Metabolic Disease
|
|
15-PGDH-IN-3 (Compound 61) is a selective competitive inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) .
|
-
- HY-N8246
-
|
Uridine-2', 3'-cyclic monophosphate sodium salt
|
Others
|
Others
|
|
2',3'-cUMP sodium (Uridine-2', 3'-cyclic monophosphate sodium salt) is a competitive inhibitor of dip-nitrophenyl diphosphate hydrolysis .
|
-
- HY-131814
-
|
|
Others
|
Others
|
|
5'-dGMPS is an analogue of 5'-dGMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dGMP .
|
-
- HY-131815
-
|
|
Others
|
Others
|
|
5'-dIMPS is an analogue of 5'-dIMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dIMP .
|
-
- HY-131813
-
|
2'-Deoxycytidine 5'-monophosphate
|
Others
|
Others
|
|
5'-dCMPS is an analogue of 5'-dCMP and a potential substrate, competitive inhibitor or regulator of enzymes that interact with 5'-dCMP .
|
-
- HY-159741
-
|
FCE 24928
|
Others
|
Cancer
|
|
Minamestane (FCE 24928) is a selective and competitive aromatase inhibitor with an IC50 value of 45.7 nM. Minamestane is promising for research of postmenopausal breast cancer .
|
-
- HY-15716
-
|
|
Ras
Apoptosis
|
Cancer
|
|
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
|
-
- HY-19712
-
LJH685
2 Publications Verification
|
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively .
|
-
- HY-14806S
-
|
MP-513 d8
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
- HY-135189
-
|
|
Others
|
Others
|
|
6-Aminophenanthridine inhibits the protein folding activity of the ribosome (PFAR). 6-Aminophenanthridine competitively occludes the protein substrates from binding to rRNA and thereby inhibits PFAR .
|
-
- HY-76409
-
|
FXV673 hydrochloride
|
Factor Xa
|
Inflammation/Immunology
|
|
Otamixaban (FXV673) is a potent, selective, rapid-acting, competitive, and reversible fXa inhibitor (Ki=0.5 nM) that effectively inhibits both free and prothrombinase-bound fXa .
|
-
- HY-155569
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 13 (compound 12g) is a non-competitive inhibitor of chitin synthase, with an IC50 of 106.7 μM. Chitin synthase inhibitor 13 exhibits a broad-spectrum of antifungal activity .
|
-
- HY-152032
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
|
-
- HY-14664AS
-
-
- HY-100005A
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity .
|
-
- HY-19548A
-
|
|
Arginase
|
Metabolic Disease
|
|
BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively .
|
-
- HY-19778
-
-
- HY-112654
-
-
- HY-N1470
-
|
|
Others
|
Metabolic Disease
|
|
Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM .
|
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-108609
-
-
- HY-116530
-
-
- HY-112405
-
|
PD 159121
|
EGFR
|
Cancer
|
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively .
|
-
- HY-17502R
-
-
- HY-120491
-
|
|
Others
|
Cardiovascular Disease
|
|
L 722151 is a competitive inhibitor for factor XIIIa with Ki of 49 µM. L 722151 accelerates tissue plasminogen activator-catalyzed clot dissolution, and exhibits antithrombotic efficacy .
|
-
- HY-N2194R
-
|
|
Cytochrome P450
|
Cancer
|
|
Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
|
-
- HY-13050A
-
|
AZD-8931 fumarate
|
EGFR
|
Cancer
|
|
Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
- HY-12964
-
|
|
TAM Receptor
|
Cancer
|
|
SGI-7079 is a potent and ATP-competitive Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
|
-
- HY-B0882S
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-Y0504R
-
|
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Trimethylammonium chloride (Standard) is the analytical standard of Trimethylammonium chloride. This product is intended for research and analytical applications. Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
|
-
- HY-121483
-
|
|
Others
|
Others
|
|
Leucinal is a competitive inhibitor of brain aminopeptidase, inhibits brain soluble aminopeptidase activity (Ki = 22 microM), and can enhance the analgesia induced by leuprorelin, but has no effect on the analgesia induced by some other substances.
|
-
- HY-148395
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
UCK2 Inhibitor-2 is a non-competitive uridine-cytidine kinase 2 (UCK2) inhibitor with an IC50 value of 3.8 µM. UCK2 Inhibitor-2 can suppress uridine salvage in cells .
|
-
- HY-15339
-
|
Cdk2 inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation .
|
-
- HY-111378
-
|
|
Casein Kinase
|
Metabolic Disease
|
|
Casein Kinase II Inhibitor IV is a potent, ATP-competitive of casein kinase II inhibitor with an IC50 of 9 nM. Casein Kinase II Inhibitor IV ia also a human keratinocytes (NHEK) differentiation inducer .
|
-
- HY-50706A
-
|
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-149425
-
|
|
Sirtuin
|
Inflammation/Immunology
Cancer
|
|
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo .
|
-
- HY-165438
-
|
|
Others
|
Others
|
|
Sergliflozin-A is a compound used to inhibit type 2 diabetes. It can inhibit glucose transporters in the kidney, competitively inhibit hSGLT1 and hSGLT2, and mutations at different sites have different effects on its inhibitory effect.
|
-
- HY-110287
-
Apcin
5 Publications Verification
|
APC
|
Cancer
|
|
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
|
-
- HY-10422
-
|
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2 .
|
-
- HY-19541
-
-
- HY-N1750
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively .
|
-
- HY-D1493
-
|
|
PKC
|
Others
|
|
FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .
|
-
- HY-118563
-
|
|
Biochemical Assay Reagents
|
Others
|
|
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
|
-
- HY-W179181
-
|
|
GLUT
|
Metabolic Disease
|
|
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. MSNBA competitively inhibits GLUT5 fructose uptake with a KI of 3.2±0.4?μM in MCF7 cells .
|
-
- HY-N2962
-
|
|
Tyrosinase
|
Inflammation/Immunology
|
|
Broussonin C is a competitive inhibitor of Tyrosinase that can be isolated from Broussonetia kazinoki. Broussonin C inhibits monophenolase and diphenolase with IC50s of 0.43 and 0.57 μM, respectively .
|
-
- HY-161137
-
|
|
Others
|
Neurological Disease
|
|
LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .
|
-
- HY-103265A
-
|
FPL 67156
|
Phosphatase
|
Others
|
|
ARL67156 is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively .
|
-
- HY-P1619
-
|
|
Others
|
Others
|
|
ICI 186756 is a compound that inhibits the activity of human neutrophil elastase, has a competitive inhibitory effect on the enzyme, can inhibit enzyme-induced lung changes, and can also modulate hamster lung lesions.
|
-
- HY-124793
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 .
|
-
- HY-124793A
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2 .
|
-
- HY-N12399
-
|
|
PKA
|
Inflammation/Immunology
|
|
Aplithianines A is a potent inhibitor against J-PKAcα with an IC50 of 1 μM , and inhibits wild-type PKA with an IC50 of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the ATP pocket .
|
-
- HY-12134
-
Poloxin
3 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
|
-
- HY-10512
-
|
AR 0133418; GSK 3β inhibitor VIII; AR 014418
|
GSK-3
|
Metabolic Disease
Cancer
|
|
AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
|
-
- HY-14711
-
|
|
Aurora Kinase
Autophagy
|
Cancer
|
|
Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
|
-
- HY-N0021
-
-
- HY-19715
-
-
- HY-14929A
-
|
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-15345
-
|
THU dihydrate; NSC-112907 dihydrate
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-112113
-
|
SEL201-88; SEL-201
|
MNK
|
Cancer
|
|
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
|
-
- HY-17502S
-
-
- HY-N0575
-
-
- HY-108643
-
|
|
MAPKAPK2 (MK2)
|
Cancer
|
|
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330?nM .
|
-
- HY-N7114A
-
|
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate sodium is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-111184
-
|
|
PI3K
|
Cancer
|
|
PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor .
|
-
- HY-15345A
-
|
THU; NSC-112907
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
|
-
- HY-119024
-
|
|
Others
|
Infection
|
|
BCI-137 is a competitive AGO2 inhibitor, with an IC50 of 342 μM. BCI-137 tightly binds to several residues of the Mid domain .
|
-
- HY-19797
-
|
|
p97
|
Cancer
|
|
ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer .
|
-
- HY-156350
-
|
|
Others
|
Cancer
|
|
SGC-STK17B-1 is an ATP-competitive and selective STK17B inhibitor (IC50: 34 nM, KD: 5.6 nM) .
|
-
- HY-105163
-
|
MPV-2213ad
|
Cytochrome P450
|
Endocrinology
|
|
Finrozole (MPV-2213ad) is a nonsteroidal, orally active and competitive aromatase enzyme inhibitor. Finrozole can be used for urinary symptoms research .
|
-
- HY-117830
-
|
|
Phosphatase
|
Endocrinology
|
|
CX08005 is a competitive PTP1B inhibitor. CX08005 can directly enhance the action of insulin in vivo and in vitro and improve insulin resistance .
|
-
- HY-111199
-
|
|
FAAH
|
Neurological Disease
|
|
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor with an IC50 of 1.6 nM in competitive activity-based protein profiling (ABPP) experiments .
|
-
- HY-157829
-
|
Me-PEA
|
Endogenous Metabolite
|
Cancer
|
|
(R)-Palmitoyl-(2-methyl)ethanolamide (Me-PEA) is a competitive inhibitor of [3 H]-AEA metabolism with a Ki value of 6.6 μM .
|
-
- HY-114991
-
|
|
HPPD
|
Others
|
|
Leptospermone is a competitive, reversible inhibitor for p-Hydroxyphenylpyruvate dioxygenase (HPPD), with an IC50 of 12.1 μM. Leptospermone exhibits herbicidal activity for its bleaching effect .
|
-
- HY-122148
-
-
- HY-18732B
-
-
- HY-18732C
-
|
Tilarginine hydrochloride; Methylarginine hydrochloride
|
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
L-NMMA (Tilarginine) hydrochloride competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA hydrochloride is utilized as NO synthase antagonist in experimental settings .
|
-
- HY-50706
-
|
AZD6244; ARRY-142886
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-10474
-
|
PP 242
|
mTOR
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM . PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively .
|
-
- HY-103261
-
|
|
Proton Pump
|
Endocrinology
|
|
SCH28080 is a reversible, K +-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity .
|
-
- HY-N2368
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-N2368A
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-137613
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
Sp-TTPαS is a competitivesterile alpha motif and HD domain containing protein 1 (SAMHD1) catalysis inhibitor. Sp-TTPαS competitively inhibits TTP hydrolysis with a Ki value of 46 µM .
|
-
- HY-19301
-
|
J-104135
|
Farnesyl Transferase
|
Cancer
|
|
J 104871 (J-104135) is a farnesyl pyrophosphate (FPP)-competitive farnesyltransferase (FTase) inhibitor. J 104871 inhibits rat brain FTase with an IC50 of 3.9 nM in the presence of farnesyl pyrophosphate (FPP) .
|
-
- HY-101169
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
|
-
- HY-N0793A
-
-
- HY-10193
-
|
|
JAK
|
Cancer
|
|
AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively .
|
-
- HY-14574
-
|
|
Aurora Kinase
VEGFR
|
Cancer
|
|
PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
|
-
- HY-B0134
-
-
- HY-100844
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM .
|
-
- HY-101760
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
|
-
- HY-12432A
-
|
ASP2215 hemifumarate
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
|
-
- HY-12806
-
|
|
EGFR
|
Cancer
|
|
AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194 .
|
-
- HY-50949A
-
|
|
IKK
|
Inflammation/Immunology
|
|
Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
|
-
- HY-115194
-
|
|
Aminopeptidase
Bacterial
|
Infection
|
|
Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase .
|
-
- HY-136548
-
-
- HY-133117A
-
|
|
IKK
|
Cancer
|
|
(Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy .
|
-
- HY-17502S1
-
-
- HY-116559
-
|
|
Others
|
Others
|
|
TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC50: 0.09 μM, Ki: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1 .
|
-
- HY-10193A
-
|
|
JAK
|
Cancer
|
|
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor .
|
-
- HY-18732
-
|
Tilarginine; Methylarginine
|
NO Synthase
|
Others
|
|
L-NMMA (Tilarginine; Methylarginine) competitively antagonizes L-arginine, and thus inhibits production of nitric oxide (NO). L-NMMA is utilized as NO synthase antagonist in experimental settings .
|
-
- HY-131811
-
|
5'-O-Thiophosphonocytidine
|
Others
|
Others
|
|
5’CMPS (5’-O-Thiophosphonocytidine) is a 5’-CMP analog that is a potential competitive inhibitor or regulator of enzymes that interact with cytidine 5’phosphate .
|
-
- HY-162909
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
Tyrosinase-IN-38 (compound 6b) is a competitive Tyrosinase inhibitor with IC50 value of 25.82 μM. Tyrosinase-IN-38 has antioxidant activity .
|
-
- HY-135404R
-
|
|
Drug Metabolite
|
Cardiovascular Disease
Cancer
|
|
Anhydrosimvastatin (Standard) is the analytical standard of Anhydrosimvastatin. This product is intended for research and analytical applications. Anhydrosimvastatin (Impurity C) is an impurity of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase .
|
-
- HY-100412A
-
|
AZD-0865 mesylate
|
Proton Pump
|
Cancer
|
|
Linaprazan mesylate can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid.
|
-
- HY-N4110
-
|
|
Cytochrome P450
NF-κB
Interleukin Related
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders .
|
-
- HY-12019
-
|
|
c-Met/HGFR
|
Cancer
|
|
SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity .
|
-
- HY-I0096
-
|
|
Endogenous Metabolite
iGluR
|
Neurological Disease
|
|
Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current .
|
-
- HY-12031A
-
|
|
MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
|
U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
|
-
- HY-125916
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity .
|
-
- HY-D0145
-
|
Resorufin ethyl ether
|
Cytochrome P450
NO Synthase
|
Others
|
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-N7763
-
|
|
Glucosidase
|
Neurological Disease
|
|
Casuarictin is a potent and competitive α-glucosidase inhibitor with an IC50 of 0.21 μg/mL. Casuarictin is a presenilin stabilization factor like protein (PSFL) protein inhibitor. Casuarictin can be used for Alzheimer's disease research .
|
-
- HY-122370A
-
|
|
Aurora Kinase
|
Cancer
|
|
Tripolin B is an ATP-competitive Aurora kinase inhibitor with IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. Tripolin B does not inhibit Aurora kinase in cells .
|
-
- HY-14660
-
|
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-15663
-
|
|
PAK
|
Cancer
|
|
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
|
-
- HY-15313
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-10458
-
|
VS-6062 besylate
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively .
|
-
- HY-15687
-
|
|
ROCK
|
Metabolic Disease
|
|
SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
|
-
- HY-15313B
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-12432
-
|
ASP2215
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-13050
-
|
AZD-8931
|
EGFR
|
Cancer
|
|
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
- HY-15313C
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-N0793
-
-
- HY-110231
-
-
- HY-124330
-
|
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively .
|
-
- HY-118660
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells .
|
-
- HY-138489
-
|
Lats-IN-1
|
YAP
|
Others
|
|
TRULI (Lats-IN-1) is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. TRULI promotes Yap-dependent proliferation in postmitotic mammalian tissues .
|
-
- HY-Y1787
-
|
|
Apoptosis
|
Neurological Disease
|
|
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis .
|
-
- HY-152194
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-10 (Compound 23) is a partially competitive tyrosinase inhibitor with an IC50 of 1.6 μM against tyrosinase activity from human melanoma cell lysates .
|
-
- HY-121966
-
|
Riparin III
|
Others
|
Cancer
|
|
Riparin is a nonspecific smooth muscle relaxant. Riparin inhibits CaCl2-induced contractions in a reversible and non-competitive manner and can be used in spasmolytic studies .
|
-
- HY-W168754
-
|
|
Others
|
Others
|
|
DB28 is a novel MR1 ligand. DB28 decreases cell surface expression of MR1 and competitively inhibits activation of MAIT cells by agonist ligands .
|
-
- HY-116208
-
|
KU-1257
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Dalcotidine (KU-1257) is an orally active and competitive histamine H2 receptor antagonist. Dalcotidine promotes the healing of chronic ulcers and inhibits gastric acid secretion .
|
-
- HY-N1201S
-
-
- HY-19156A
-
|
ICI-D 6888 hydrochloride
|
Angiotensin Receptor
|
Others
|
|
ZD-6888 hydrochloride (ICI-D 6888 hydrochloride) is an antagonist for angiotensin II, which competitively inhibits the angiotensin II-mediated release of renin, affects the renal structure and function .
|
-
- HY-117595
-
|
|
FAK
FGFR
Apoptosis
|
Cancer
|
|
PHM16 is an ATP competitive inhibitor of FAK and FGFR2 (IC50: 0.4 μM and 0.37 μM, respectively), with direct potent anti-angiogenic activity .
|
-
- HY-13450
-
|
|
JAK
EGFR
|
Inflammation/Immunology
|
|
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3 .
|
-
- HY-N1860
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
3-O-Methylquercetin (3-MQ) is a major component from the plant Rhamnus nakaharai and has antiviral activity and potential antiasthmatic efficacy. 3-O-Methylquercetin inhibits total cAMP and cGMP-phosphodiesterase (PDE). The IC50 values of 3-O-Methylquercetin (3-MQ) against PDE1-PDE5 are in the range of 1.6-86.9 μM. 3-O-Methylquercetin is a non-competitive inhibitor of PDE2 and a competitive inhibitor of PDE4 .
|
-
- HY-12054
-
|
|
Aurora Kinase
Autophagy
Influenza Virus
Parasite
|
Cancer
|
|
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral .
|
-
- HY-100472
-
|
|
Caspase
|
Cancer
|
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3 .
|
-
- HY-121377
-
-
- HY-153629
-
|
|
Ferroptosis
|
Cancer
|
|
FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer .
|
-
- HY-N2368B
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake .
|
-
- HY-N10002
-
|
|
Phosphatase
Glucosidase
|
Metabolic Disease
|
|
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes .
|
-
- HY-146154
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers .
|
-
- HY-70044
-
|
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-10459
-
|
VS-6062
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-100011
-
SR-3029
2 Publications Verification
|
Casein Kinase
|
Cancer
|
|
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
|
-
- HY-100412
-
|
AZD0865
|
Proton Pump
|
Cancer
|
|
Linaprazan (AZD0865) can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid.
|
-
- HY-114702
-
M77976
1 Publications Verification
|
PDHK
|
Metabolic Disease
|
|
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes .
|
-
- HY-20403
-
|
VS-6062(hydrochloride)
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-16958
-
|
|
Antibiotic
|
Inflammation/Immunology
|
|
PD 404182 is a potent and competitive inhibitor of human dimethylarginine dimethylaminohydrolase 1 (DDAH1), with an IC50 of 9 μM. PD 404182 exhibits antiangiogenic and antiviral activity in vitro .
|
-
- HY-136548A
-
|
TFV-DP triethylamine
|
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT) .
|
-
- HY-15159
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases .
|
-
- HY-79457
-
|
|
NO Synthase
HSV
|
Infection
Inflammation/Immunology
|
|
S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock .
|
-
- HY-119611A
-
-
- HY-B0199A
-
|
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Endogenous Metabolite
Bacterial
|
Cancer
|
|
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-115740
-
|
Ara-CTP
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytarabine triphosphate (Ara-CTP), an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
|
-
- HY-151150
-
|
|
Parasite
|
Infection
|
|
Trypanothione synthetase-IN-2 (Compound 3) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 5.4 μM when triamine spermidine is as polyamine S .
|
-
- HY-151148
-
|
|
Parasite
|
Infection
|
|
Trypanothione synthetase-IN-1 (Compound 1) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 14.8 μM when triamine spermidine is as polyamine S .
|
-
- HY-139196
-
-
- HY-W012888
-
|
(-)-Leucinol
|
Others
|
Others
|
|
D-Leucinol is the isomer of L-Leucinol (HY-W015876), and can be used as an experimental control. L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM .
|
-
- HY-155837
-
|
|
Others
|
Metabolic Disease
|
|
hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
|
-
- HY-N9685
-
|
D-(+)-Digitoxose
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Digitoxose (D-(+)-Digitoxose), a natural product, specifically and competitively inhibits glucose-stimulated insulin release from islets in lean and obese mice. Digitoxose can be used in diabetes research .
|
-
- HY-103366
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer .
|
-
- HY-120650
-
|
|
FAAH
|
Infection
|
|
CAY10435 is a β-ketooxazapyridine, selective FAAH inhibitor with antimicrobial activity. CAY10435 binds non-competitively to the FAAH of Dictyostelium discoideum with a Kd value of 0.57 nM .
|
-
- HY-W010510R
-
|
|
Endogenous Metabolite
Arginase
|
Metabolic Disease
|
|
DL-Norvaline (Standard) is the analytical standard of DL-Norvaline. This product is intended for research and analytical applications. DL-Norvaline, a derivative of L-norvaline, L-norvaline is a non-competitive inhibitor of arginase.
|
-
- HY-13100A
-
|
|
Others
|
Metabolic Disease
|
|
(S)-PF 03716556 is a K+-competitive acid blocker with gastric acid pump inhibitory activity. (S)-PF 03716556 can be used to inhibit disease states mediated by acid pump inhibitory activity .
|
-
- HY-146387
-
|
|
Sirtuin
|
Neurological Disease
Cancer
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases .
|
-
- HY-100846
-
JQEZ5
3 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects .
|
-
- HY-A0166
-
|
MK0791
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-14806B
-
|
MP-513 hydrobromide hydrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin hydrobromide hydrate is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
|
-
- HY-133125
-
|
|
Others
|
Inflammation/Immunology
|
|
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates .
|
-
- HY-A0166A
-
|
MK0791 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct .
|
-
- HY-100397
-
|
|
Elastase
|
Inflammation/Immunology
|
|
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
|
-
- HY-113054
-
|
|
Acyltransferase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase .
|
-
- HY-103566
-
|
|
mGluR
EGFR
|
Neurological Disease
|
|
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM .
|
-
- HY-129682
-
-
- HY-110335
-
|
|
ROCK
|
Cancer
|
|
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
|
-
- HY-117923
-
|
|
mTOR
PI3K
|
Cancer
|
|
PF-06465603 is a highly potent and selective ATP-competitive kinase inhibitor and a class 1 PI3K and mTOR inhibitor. PF-06465603 is a metabolite of PF-04691502 with a terminal carboxylic acid structure .
|
-
- HY-B0879
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-15513
-
|
|
DAPK
|
Cancer
|
|
TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
|
-
- HY-B0418A
-
|
R-18553 hydrochloride
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-13462
-
|
HTS466284
|
TGF-β Receptor
|
Cancer
|
|
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II .
|
-
- HY-15186A
-
|
GDC-0068 dihydrochloride; RG-7440 dihydrochloride
|
Organoid
Akt
|
Cancer
|
|
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
|
-
- HY-103384
-
|
|
Casein Kinase
|
Cancer
|
|
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
|
-
- HY-134274
-
|
8-Bromoguanosine-5'-triphosphate
|
Bacterial
|
Infection
|
|
8-Br-GTP, a GTP analog, is a competitive FtsZ polymerization and GTPase activity (Ki of 31.8 μM) inhibitor. 8-Br-GTP can be used for nucleic acid modification .
|
-
- HY-115887
-
-
- HY-126730
-
|
|
Phosphatase
|
Cancer
|
|
Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
|
-
- HY-N6054
-
|
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-14929
-
|
GR181413A free base
|
Others
|
Others
|
|
Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A .
|
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Glucosidase
|
Metabolic Disease
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
|
-
- HY-153320
-
|
|
MAP3K
|
Cancer
|
|
AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines .
|
-
- HY-P4633
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet .
|
-
- HY-N1201R
-
|
4',5,7-Trihydroxyflavone(Standard); Apigenol(Standard); C.I. Natural Yellow 1 (Standard)
|
Autophagy
Cytochrome P450
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
|
-
- HY-N12736
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Dehydrodanshenol A is a non-competitive inhibitor of Protein tyrosine phosphatase 1B (PTP1B), with an IC50 value of 8.5 μM. Dehydrodanshenol A can be used in diabetes-related research .
|
-
- HY-20558R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-(+)-Malic acid (Standard) is the analytical standard of D-(+)-Malic acid. This product is intended for research and analytical applications. D-(+)-Malic acid (D-Malic acid), an active enantiomer of Malic acid, is a competitive inhibitor of L(--)malic acid transport .
|
-
- HY-N9949
-
|
Lupinidine
|
nAChR
|
Neurological Disease
|
|
Sparteine (Lupinidine) is an alkaloid compound derived from leguminous plants and can act as a ganglionic blocker. Sparteine competitively inhibits the activity of the neuronal nicotinic acetylcholine receptor (nACh receptor) .
|
-
- HY-13503R
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Epothilone A (Standard) is the analytical standard of Epothilone A. This product is intended for research and analytical applications. Epothilone A is a competitive inhibitor of the binding of [3H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM.
|
-
- HY-135072R
-
|
|
Others
|
Infection
|
|
N,N',N''-Triacetylchitotriose (Standard) is the analytical standard of N,N',N''-Triacetylchitotriose. This product is intended for research and analytical applications. N,N',N''-Triacetylchitotriose is a competitive inhibitor of lysozyme .
|
-
- HY-10531
-
|
|
EGFR
|
Cancer
|
|
ARRY-380 analog, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249 . ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2 .
|
-
- HY-10163
-
|
BIBR 953; BIBR 953ZW
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-103316A
-
Ned 19
2 Publications Verification
|
Calcium Channel
|
Cancer
|
|
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
|
-
- HY-10787
-
|
H 376/95
|
Thrombin
|
Cardiovascular Disease
|
|
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics .
|
-
- HY-10255A
-
|
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-10917
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-100616
-
|
cis-1-Aminocyclobutane-1,3-dicarboxylic acid
|
Others
|
Neurological Disease
|
|
cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasma membrane glutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
|
-
- HY-19981
-
|
ARQ-087
|
FGFR
|
Cancer
|
|
Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
|
-
- HY-108935
-
|
|
HIV Integrase
GLUT
Tyrosinase
|
Cancer
|
|
Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases .
|
-
- HY-145860
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
|
-
- HY-19981B
-
|
ARQ-087 dihydrochloride
|
EGFR
|
Cancer
|
|
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
|
-
- HY-122011
-
|
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
|
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration .
|
-
- HY-14806A
-
|
MP-513 hydrobromide
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
|
-
- HY-12832
-
-
- HY-108333
-
|
|
Tie
BRK
|
Cardiovascular Disease
Cancer
|
|
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis .
|
-
- HY-126015
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator .
|
-
- HY-116750
-
|
|
Tyrosinase
|
Others
|
|
6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .
|
-
- HY-149929
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7 .
|
-
- HY-147342
-
|
|
Others
|
Others
|
|
β-Benzamide adenine dinucleotide is a bioactive metabolite of benzamide nucleoside and a potent inhibitor of inosine 5 '-monophosphate dehydrogenase (IMPDH). β-Benzamide adenine dinucleotide is a potent, competitive inhibitor of human NAD kinase (Ki = 90 µM) .
|
-
- HY-158987
-
|
APBADP
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Adenosine phosphonobutyric, 2'(3'), 5'-diposphate (APBADP) is a potent Bacillus subtilis and human adenylosuccinate lyase (ASL) inhibitor. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate also is a competitive succinylaminoimidazole carboxamide ribotide (SAICAR) inhibitor .
|
-
- HY-13558
-
|
SH 489
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH) .
|
-
- HY-146318
-
-
- HY-16082
-
AZD7545
1 Publications Verification
|
PDHK
|
Metabolic Disease
|
|
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively .
|
-
- HY-B0334
-
|
CP45899
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
|
-
- HY-13217
-
|
GBR-12909 dihydrochloride; I893 dihydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT) .
|
-
- HY-13217A
-
|
GBR 12909; I893
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT) .
|
-
- HY-12293
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
|
-
- HY-12493A
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-N6650
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.
|
-
- HY-B0165CS
-
-
- HY-101190
-
-
- HY-N4289
-
|
|
Cathepsin
|
Cancer
|
|
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B .
|
-
- HY-12493B
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-12853
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-B0334A
-
|
CP45899 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
|
-
- HY-119611
-
-
- HY-151115
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
JNJ-1289 is a potent, selective, competitive and allosteric human spermine oxidase (hSMOX) inhibitor (IC50: 50 nM). JNJ-1289 can be used in the research of polyamine catabolism, inflammation and cancers .
|
-
- HY-N10497
-
|
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced .
|
-
- HY-148207
-
|
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-Benzylglutathione is a competitive glutathionase inhibitor. S-Benzylglutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-Benzylglutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system .
|
-
- HY-N7114
-
|
|
Antibiotic
Bacterial
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate also is an antibiotic. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-121908
-
|
|
ATP Synthase
|
Cancer
|
|
FCPT, an ATP competitive inhibitor, induces a tight-binding of kinesin-5 onto microtubules and induced loss of microtubules selectively at the poles of Xenopus extract spindles without altering microtubule dynamics .
|
-
- HY-149711
-
|
|
ICMT
|
Metabolic Disease
|
|
Farnesylcysteine (FC) is a competitive inhibitor of ICMT. The fcly mutant has quantitatively low farnesylcysteine (FC) lyase activity and an enhanced response to ABA. Farnesylcysteine induces an ABA hypersensitive phenotype in Arabidopsis thaliana .
|
-
- HY-115740A
-
|
Ara-CTP trisodium
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytarabine triphosphate (Ara-CTP) trisodiu, an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate trisodiu levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
|
-
- HY-122200
-
|
JS399-19
|
Myosin
Fungal
|
Infection
|
|
Phenamacril (JS399-19) inhibits activity of myosin I non-competitively with an IC50 of 360 nM through suppression of the ATPase activity, exhibits therefore an antifungal efficacy towards Fusarium species .
|
-
- HY-B0183R
-
-
- HY-123665
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PSB-1410 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with IC50 for human MAO-B and rat MAO-B Values are 0.23 and 1.01 nM respectively .
|
-
- HY-P2477
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
|
-
- HY-112390A
-
|
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-112390
-
|
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-112390C
-
|
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II hydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II hydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II hydrochloride shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-B0879A
-
|
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-11001
-
|
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-50846
-
|
|
ERK
|
Cancer
|
|
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations .
|
-
- HY-112136
-
|
CP 43
|
MAP3K
|
Cancer
|
|
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death .
|
-
- HY-110156
-
|
|
Others
|
Cancer
|
|
Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM .
|
-
- HY-12031
-
|
|
MEK
Autophagy
Mitophagy
Influenza Virus
|
Cancer
|
|
U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor .
|
-
- HY-18963
-
|
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
|
-
- HY-125017
-
|
PLB-1001; CBT-101; Vebreltinib
|
c-Met/HGFR
|
Cancer
|
|
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily .
|
-
- HY-136270
-
|
VX-803; M4344; ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
|
-
- HY-112401
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
|
-
- HY-147823
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-6 (compound 18) is a competitive α-glucosidase inhibitor with an IC50 of 5.69 µM. α-Glucosidase-IN-6 has anti-diabetic potential .
|
-
- HY-11087
-
|
SD-06
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α .
|
-
- HY-12012
-
-
- HY-13994
-
|
|
Mps1
Polo-like Kinase (PLK)
|
Cancer
|
|
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
|
-
- HY-12774
-
IC261
4 Publications Verification
|
Casein Kinase
Apoptosis
|
Cancer
|
|
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
|
-
- HY-101212
-
|
CYC065
|
CDK
|
Cancer
|
|
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively .
|
-
- HY-100888
-
|
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity .
|
-
- HY-59090
-
-
- HY-118047
-
-
- HY-112468
-
|
|
CDK
|
Cancer
|
|
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively .
|
-
- HY-10963
-
|
CYT387 mesylate
|
JAK
Autophagy
|
Cancer
|
|
Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
|
-
- HY-117319
-
|
TAK-083; PA-155A
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA synthetase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity .
|
-
- HY-W015514
-
|
|
Others
|
Neurological Disease
|
|
N-(3-Aminopropyl)cyclohexylamine, a cyclohexylamine derivative, acts as a selective and competitive inhibitor of spermine synthase. N-(3-Aminopropyl)cyclohexylamine can be used for the research of neurological diseases .
|
-
- HY-N10488
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC50 of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research .
|
-
- HY-155970
-
-
- HY-155973
-
-
- HY-114503A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-W727627
-
|
|
Amylases
|
Metabolic Disease
|
|
5-O-Coumaroylquinic acid is a potent, reversible, non-competitive α-amylase inhibitor with an IC50 value of 69.39 μM. 5-O-Coumaroylquinic acid can be used in diabetes research .
|
-
- HY-N9075
-
|
|
Glucosidase
|
Cancer
|
|
9-(4′-Hydroxyphenyl)-2-methoxyphenalen-1-one is a phytoalexin and mixed competitive α-glucosidase inhibitor of Bacillus stearothermophilus (IC50: 3.86 mg/L) .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-10255
-
|
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-17423
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-18780
-
RR6
2 Publications Verification
|
Others
|
Cancer
|
|
RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively .
|
-
- HY-13634B
-
-
- HY-P0222
-
|
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-W051513
-
|
|
PARP
|
Others
|
|
2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM .
|
-
- HY-17423E
-
|
|
HIV
Apoptosis
Reverse Transcriptase
Telomerase
|
Infection
Cancer
|
|
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-B0873
-
|
|
Cytochrome P450
ROS Kinase
|
Others
|
|
Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent .
|
-
- HY-124366
-
|
|
Others
|
Infection
Cancer
|
|
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
|
-
- HY-145418
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .
|
-
- HY-145419
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .
|
-
- HY-145420
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .
|
-
- HY-147875
-
|
|
Aldose Reductase
|
Metabolic Disease
|
|
Aldose reductase-IN-6 (Compound 3) is a competitive aldose reductase (AR) inhibitor with an IC50 of 3.164 μM and a Ki of 0.018 μM. Aldose reductase-IN-6 exhibits no cytotoxicity against healthy cells .
|
-
- HY-118795
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis .
|
-
- HY-155030
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-25 (Compound (R)-8k) is a competitive inhibitor of α-glucosidase, with an IC50 of 1.19μM and can be used for anti-diabetic research .
|
-
- HY-10319
-
BAY-549
2 Publications Verification
ROCK-IN-2; Azaindole 1; TC-S 7001
|
ROCK
|
Cardiovascular Disease
|
|
BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively .
|
-
- HY-14691
-
|
BAY 869766; RDEA119
|
MEK
|
Cancer
|
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-18930
-
|
|
CDK
|
Cancer
|
|
NU6300 is a covalent, irreversible and ATP-competitive CDK2 inhibitor with an IC50 value of 0.16 μM. NU6300 can be used for the research of eukaryotic cell cycle- and transcription-related .
|
-
- HY-12866
-
|
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-U00448
-
|
|
Others
|
Cancer
|
|
ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
|
-
- HY-112668
-
|
SP2086 phosphate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research .
|
-
- HY-16446
-
|
|
c-Met/HGFR
PI3K
Akt
MEK
Apoptosis
|
Cancer
|
|
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer .
|
-
- HY-113514
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
6-Phosphogluconic acid is a potent and competitive phosphoglucose isomerase (PGI) inhibitor with Kis of 48 μM for glucose 6-phosphate and 42 μM for fructose 6-phosphate. 6-Phosphogluconic acid is an endogenous metabolite .
|
-
- HY-12493
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
|
-
- HY-112668A
-
|
SP2086
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) research .
|
-
- HY-139253
-
-
- HY-10515
-
|
|
PDK-1
|
Cancer
|
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect .
|
-
- HY-155374
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer .
|
-
- HY-157132
-
|
|
FAAH
|
Neurological Disease
|
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
|
-
- HY-161299
-
|
|
Parasite
|
Infection
|
|
LAPTc-IN-1 (compound 4) is a competitive inhibitor targeting acidic M17 leucinopeptidase (LAPTc) with Ki=0.27 μM. LAPTc-IN-1 is a potential antagonist of the parasite Trypanosoma cruzi .
|
-
- HY-116097
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .
|
-
- HY-B0165S
-
-
- HY-122060
-
|
|
NO Synthase
|
Metabolic Disease
|
|
BYK 191023 is a selective and L-arginine competitive inducible nitric-oxide synthase inhibitor with an IC50 value of 86 nM, 17 µM, 162 µM for inducible (iNOS), neuronal (nNOS), and endothelial (eNOS) NO synthases respectively .
|
-
- HY-135405R
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
4-Acetylsimvastatin (Standard) is the analytical standard of 4-Acetylsimvastatin. This product is intended for research and analytical applications. 4-Acetylsimvastatin is an acetylated simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM .
|
-
- HY-W685943
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Heptaminol is a fatty amine with pressor properties and a potential antihypotension agent. Heptaminol is also a competitive inhibitor of norepinephrine uptake and an inhibitor of nicotine-induced catecholamine release (IC50: 650 μM). Heptaminol does not inhibit norepinephrine release induced by 59 mM K + but rather inhibits high-affinity Na +-dependent norepinephrine uptake .
|
-
- HY-112390B
-
|
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect .
|
-
- HY-13945
-
NVP 231
2 Publications Verification
|
Apoptosis
|
Cancer
|
|
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .
|
-
- HY-10195B
-
|
LY333531 hydrochloride
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM .
|
-
- HY-18990
-
|
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-103021
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent .
|
-
- HY-10195
-
|
LY333531
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM .
|
-
- HY-150761
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity .
|
-
- HY-13966S
-
|
2-DG-d1; 2-Deoxy-D-arabino-hexose-d1; D-Arabino-2-deoxyhexose-d1
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-101920
-
|
|
Autophagy
PI3K
|
Neurological Disease
Cancer
|
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34 .
|
-
- HY-W009156
-
-
- HY-Y0413
-
|
Diacetyl monoxime; DAM
|
Na+/K+ ATPase
Myosin
|
Metabolic Disease
|
|
Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca 2+ release .
|
-
- HY-112349
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB 203580 sulfone is an analog of p38 MAP kinase inhibitor SB 203580, which inhibits the IL-1 production in monocytes with an IC50 of 0.2 μM and binds competitively with CSAID binding proteins (CSBP), inhibits it mediated stress response signaling with an IC50 of 0.03 μM .
|
-
- HY-11003
-
|
GW843682
|
Polo-like Kinase (PLK)
|
Cancer
|
|
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.
|
-
- HY-10961
-
|
CYT387
|
JAK
Autophagy
Apoptosis
|
Cancer
|
|
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
|
-
- HY-B0574
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-15272
-
|
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
- HY-100714A
-
|
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors .
|
-
- HY-W015309S
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-16007
-
|
Garcinia acid
|
ATP Citrate Lyase
|
Metabolic Disease
|
|
(-)-Hydroxycitric acid (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia. (-)-Hydroxycitric acid is a potent and competitive and orally active inhibitor of ATP citrate lyase. (-)-Hydroxycitric acid suppresses the fatty acid synthesis, lipogenesis, food intake, and induced weight loss .
|
-
- HY-10716A
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-113468A
-
|
3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
|
-
- HY-W015309S2
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-115062
-
|
|
Phospholipase
|
Metabolic Disease
|
|
MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-14117
-
-
- HY-W015309S1
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-W015309S3
-
|
|
iGluR
|
Neurological Disease
|
|
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-111173
-
|
|
Dipeptidyl Peptidase
|
Others
|
|
Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
|
-
- HY-100786
-
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Ser/Thr Protease
|
Cancer
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-149477
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
IHC3 is a competitive and reversible MAO-B inhibitor (IC50: 1.672 μM). IHC3 can interact with the amino acid Cys172 of MAO-B. IHC3 can be used for neurological diseases research .
|
-
- HY-156136
-
|
|
Biochemical Assay Reagents
|
Others
|
|
5-n-Heptyl-6-hydroxy-4,7-dioxobenzothiazole is a competitive Qo site inhibitor of the cytochrome bc 1 complex (cytochrome c oxidoreductase) from Saccharomyces cerevisiae .
|
-
- HY-162139
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Urease-IN-11 (Compound 6e) is a competitive urease inhibitor (IC50)=10.41 µM). Urease-IN-11 can be used to study diseases such as urease-related gastritis and peptic ulcer .
|
-
- HY-116392B
-
|
|
Glucosylceramide Synthase (GCS)
|
Cancer
|
|
DL-threo-PDMP hydrochloride is the hydrochloride form of DL-threo-PDMP that is a competitive glucosylceramide synthase (GCS) inhibitor. DL-threo-PDMP resensitizes refractory testicular germ cell tumors and epithelial ovarian cancer orthoxenografts to cisplatin in mice .
|
-
- HY-131817
-
|
|
Others
|
Others
|
|
5'-GMPS is an analogue of 5'-GMP and a substrate, competitive inhibitor or regulator of enzymes that interact with 5'-GMP. 5'-GMPS is suitable as a primer of RNA synthesis by T7 RNA polymerase .
|
-
- HY-W039920
-
|
β-D-Galactosylamine, 98%
|
Biochemical Assay Reagents
|
Others
|
|
1-Amino-1-deoxy-β-D-galactose, 98% is a galactose analog used as a competitive inhibitor to aid in the separation, purification, identification, differentiation, and characterization of β-D-galactosidase and galactose oxidase.
|
-
- HY-10716
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research .
|
-
- HY-113850
-
|
|
Others
|
Neurological Disease
Cancer
|
|
CPSA is a potent and competitive inhibitor against 20α-hydroxysteroid dehydrogenase (AKR1C1) with a Ki value of 0.86 nM. CPSA is promising for research of lung and endometrial cancers, premature birth and neuronal disorders .
|
-
- HY-101549A
-
|
UNC2371 hydrochloride
|
FLT3
|
Cancer
|
|
MRX-2843 hydrochloride is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-17537
-
|
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
|
-
- HY-12275
-
|
|
Flavivirus
Dengue virus
ERK
Apoptosis
|
Cancer
|
|
FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively .
|
-
- HY-108540
-
|
2-Amino-2-norbornanecarboxylic acid; LAT1-IN-1
|
Apoptosis
|
Cancer
|
|
BCH (2-Amino-2-norbornanecarboxylic acid) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis .
|
-
- HY-P0222A
-
|
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-W011834
-
|
|
HCV
|
Infection
|
|
2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
|
-
- HY-N1193
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sulfuretin inhibits the inflammatory response by suppressing the NF-κB pathway. Sulfuretin can be used for the research of allergic airway inflammation. Sulfuretin reduces oxidative stress, platelet aggregation, and mutagenesis . Sulfuretin is a competitive and potent inhibitor of monophenolase and diphenolase activities with the IC50 of 13.64 μM .
|
-
- HY-118131
-
|
|
Ser/Thr Protease
|
Infection
|
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages .
|
-
- HY-129137
-
|
Cy 3-soph
|
Others
|
Others
|
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-105336
-
|
NSC 126849
|
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3-Deazauridine (NSC 126849) is a uridine analogue. 3-Deazauridine competitively inhibits cytidine triphosphate synthase to inhibit the biosynthesis of cytidine-5'-triphosphate. 3-Deazauridine acts synergistically with several antineoplastic agents, acting as a biological response modifier .
|
-
- HY-110150
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
|
-
- HY-B0879AR
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-10255AS
-
|
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-122866
-
|
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
|
-
- HY-10337
-
|
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β .
|
-
- HY-70072
-
|
|
Phospholipase
|
Infection
Inflammation/Immunology
Cancer
|
|
D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity .
|
-
- HY-14281
-
|
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-15687A
-
|
|
ROCK
|
Metabolic Disease
|
|
SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
|
-
- HY-12219
-
|
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-19794
-
|
|
SphK
|
Cancer
|
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
|
-
- HY-12219A
-
|
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-100888A
-
|
(R)-TAK-931
|
Others
|
Others
|
|
(R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM .
|
-
- HY-101445A
-
|
|
Tyrosinase
|
Cancer
|
|
(R)-Trolox is a vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM . The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM) .
|
-
- HY-12122A
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM . AR-C102222 hydrochloride has antinociception and anti-inflammatory activities .
|
-
- HY-15260
-
XL413
4 Publications Verification
BMS-863233
|
CDK
|
Cancer
|
|
XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
|
-
- HY-108605
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a Ki of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds .
|
-
- HY-111237
-
|
Olomoucin
|
CDK
|
Cancer
|
|
Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus . Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines .
|
-
- HY-12432S1
-
|
ASP2215-d8
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-B0690
-
-
- HY-W011184
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
6-Phosphogluconic acid trisodium is a potent and competitive phosphoglucose isomerase (PGI) inhibitor with Kis of 48 μM for glucose 6-phosphate and 42 μM for fructose 6-phosphate. 6-Phosphogluconic acid trisodium is an endogenous metabolite .
|
-
- HY-15251A
-
|
(Rac)-Repertaxin; (Rac)-DF 1681Y
|
Others
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
(Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-B0183S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). Ellagic acid is a natural antioxidant and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM .
|
-
- HY-19548
-
|
|
Arginase
|
Endocrinology
|
|
BEC, an arginine analogue, is a slow-binding competitive inhibitor of the binuclear manganese metalloenzyme arginase. BEC enhances substrate flux to NO synthase, thereby enhancing NO-dependent smooth muscle relaxation in the corpus cavernosum, and enhances penile erection .
|
-
- HY-126946
-
|
|
Fungal
|
Infection
|
|
Nikkomycin pseudo-J is a tripeptide derivative of the nikkomycin class found in Streptomyces tendae, which has antifungal and antiinsect activities. Nikkomycin pseudo-J exerts its biological activity by competitively inhibiting chitin synthetase of fungi and insects .
|
-
- HY-123199
-
|
SABA
|
Serotonin Transporter
|
Neurological Disease
|
|
Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
|
-
- HY-B1295
-
-
- HY-W015445
-
|
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
|
-
- HY-B2152
-
|
Hemicholinium dibromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh) . Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [ 3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively .
|
-
- HY-W129596
-
|
|
Virus Protease
|
Infection
|
|
Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability .
|
-
- HY-161913
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC50 values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively .
|
-
- HY-15473
-
|
ML120B
|
IKK
|
Cancer
|
|
MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis .
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-16569S
-
-
- HY-16569S1
-
-
- HY-13816
-
|
|
CDK
ATM/ATR
|
Cancer
|
|
NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner .
|
-
- HY-15473A
-
|
ML120B dihydrochloride
|
IKK
|
Inflammation/Immunology
Cancer
|
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis .
|
-
- HY-13966S2
-
|
2-DG-13C; 2-Deoxy-D-arabino-hexose-13C; D-Arabino-2-deoxyhexose-13C
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose- 13C is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-139158
-
|
|
HIV
|
Infection
|
|
Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-W661499
-
|
|
Phosphatase
|
Cancer
|
|
Orellanine is a fungal nephrotoxin. Orellanine is also a competitive inhibitor of alkaline phosphatase. Orellanine induces cell death in proximal tubular cells and in ccRCC cells. Orellanine can be used for research of clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-10721
-
|
AKT protein kinase inhibitor
|
Akt
|
Cancer
|
|
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
|
-
- HY-P0322
-
|
EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-101549
-
|
UNC2371
|
FLT3
|
Cancer
|
|
MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively .
|
-
- HY-135878
-
|
|
Adenylate Cyclase
Adrenergic Receptor
|
Metabolic Disease
|
|
2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart .
|
-
- HY-132309
-
BRD0639
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
|
-
- HY-112532
-
|
|
Leukotriene Receptor
Lipoxygenase
|
Inflammation/Immunology
|
|
REV 5901 is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 is also a 5-lipoxygenase inhibitor. REV 5901 can be used for the research of asthma in which leukotriene release be involved .
|
-
- HY-B0231A
-
|
MK-422 anhydrous
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat (MK-422 anhydrous), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat can be used for the research of hypertension .
|
-
- HY-122289
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
|
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
|
-
- HY-15345AS
-
|
THU-d3; NSC-112907-d3
|
Isotope-Labeled Compounds
|
Cancer
|
|
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
|
-
- HY-157124
-
|
|
Tyrosinase
|
Metabolic Disease
|
Tyrosinase-IN-19 (compound 9) is a competitive tyrosinase inhibitor. Tyrosinase-IN-19 has strong antioxidant activities against ROS, ABTS+, and DPPH radicals. Tyrosinase-IN-19 suppresses tyrosinase expression in a dose-dependent manner .
|
-
- HY-111095S2
-
|
(R)-2-Hydroxypropionic acid-13C-1; D-Lactic acid-13C-1
|
Endogenous Metabolite
|
Others
|
|
D-(-)-Lactic acid- 13C-1 is the 13C labeled D-(-)-Lactic acid. D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants .
|
-
- HY-20696R
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
Tetrahydro-β-carboline (Standard) is the analytical standard of Tetrahydro-β-carboline. This product is intended for research and analytical applications. Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 μM .
|
-
- HY-N0021R
-
|
|
PKC
Apoptosis
Bacterial
HSV
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Verbascoside (Standard) is the analytical standard of Verbascoside. This product is intended for research and analytical applications. Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
|
-
- HY-N0575R
-
|
|
Bacterial
Reactive Oxygen Species
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
|
Pinocembrin (Standard) is the analytical standard of Pinocembrin. This product is intended for research and analytical applications. Pinocembrin ((+)-Pinocoembrin) is a flavonoid found in propolis, acts as a competitive inhibitor of histidine decarboxylase, and is an effective anti-allergic agent, with antioxidant, antimicrobial and anti-inflammatory properties .
|
-
- HY-100824
-
|
|
Src
|
Cancer
|
|
PP2 Analog (compound 3) is a ATP-competitive Src family kinases inhibitor with the IC50 values of 0.22, 0.15, 2.68, and 7 aganist of lck (64-509), src , kdr, and tie-2 .
|
-
- HY-118086
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
MRS 1067 is a competitive antagonist of the adenosine A3 receptor that inhibits the suppression of adenylate cyclase by adenosine A3 receptor agonists and affects the activation of G proteins. MRS 1067 can be used in research related to inflammation and cancer .
|
-
- HY-112532A
-
|
|
Leukotriene Receptor
Lipoxygenase
|
Inflammation/Immunology
|
|
REV 5901 hydrochloride is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 hydrochloride is also a 5-lipoxygenase inhibitor. REV 5901 hydrochloride can be used for the research of asthma in which leukotriene release be involved .
|
-
- HY-10255AS1
-
|
|
Isotope-Labeled Compounds
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-10253
-
AG1024
5 Publications Verification
Tyrphostin AG 1024
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity .
|
-
- HY-125833
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
Apoptosis
|
Cancer
|
|
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis .
|
-
- HY-136532
-
ZT-1a
1 Publications Verification
|
Others
|
Neurological Disease
|
|
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively .
|
-
- HY-135780
-
-
- HY-30008
-
|
|
iGluR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects .
|
-
- HY-15003
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects .
|
-
- HY-D0145S
-
|
Resorufin ethyl ether-d5
|
Isotope-Labeled Compounds
Cytochrome P450
NO Synthase
|
Others
|
|
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
|
-
- HY-17423B
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-114730
-
|
|
IKK
|
Inflammation/Immunology
|
|
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
|
-
- HY-128041
-
|
Hydroxyfarnesyl phosphate
|
Others
|
Others
|
|
α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.
|
-
- HY-103353
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-107001
-
|
(S)-DPC 961; DMP 961
|
HIV
Reverse Transcriptase
|
Infection
|
|
DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS .
|
-
- HY-11005
-
BX-912
4 Publications Verification
|
PDK-1
Apoptosis
|
Cancer
|
|
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
|
-
- HY-10403
-
-
- HY-111383
-
-
- HY-13965
-
|
ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
|
-
- HY-121515
-
|
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property .
|
-
- HY-121515A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property .
|
-
- HY-150207
-
|
|
PARP
|
Inflammation/Immunology
|
|
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation .
|
-
- HY-N8382
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
|
-
- HY-160564
-
|
|
EGFR
|
Cancer
|
|
ZNL-0056 is an orally active ATP-competitive inhibitor that targets both the Cys797 and Cys775 in the ATP binding site of EGFR. ZNL-0056 selectively inhibits EGFR and its downstream signaling in H3255 cells. ZNL-0056 can be used for the research of cancer .
|
-
- HY-138813A
-
|
(E/Z)-SU-12662 hydrochloride
|
Others
|
Cancer
|
|
(E/Z)-N-Desethylsunitinib hydrochloride ((E/Z)-SU-12662 hydrochloride) is a compound with potential anti-tumor activity that inhibits VEGF-R2 and PDGF-Rβ tyrosine kinases. (E/Z)-N-Desethylsunitinib hydrochloride is the main active metabolite of sunitinib and has the ability to competitively inhibit ATP .
|
-
- HY-Y0978S2
-
|
N-tert-Butoxycarbonyl-2-aminoacetic acid-2-13C; NSC 127669-2-13C
|
Isotope-Labeled Compounds
Androgen Receptor
|
Endocrinology
|
|
Boc-Glycine-2- 13C is a 13C-labeled Linuron. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive a
|
-
- HY-B0134R
-
|
|
Aminopeptidase
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Bestatin (Standard) is the analytical standard of Bestatin. This product is intended for research and analytical applications. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
|
-
- HY-10962
-
|
CYT387 sulfate salt
|
JAK
Autophagy
Apoptosis
|
Cancer
|
|
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
|
-
- HY-B0231
-
|
MK-422
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat dihydrate (MK-422), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension .
|
-
- HY-18237
-
|
|
Src
|
Others
|
|
KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC50 of 40 μM. KX1-004 protects the cochlea from hazardous noise and prevents noise-induced hearing loss (NIHL) .
|
-
- HY-10079
-
CHS-828
1 Publications Verification
GMX1778
|
NAMPT
Apoptosis
|
Cancer
|
|
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
|
-
- HY-12492
-
|
|
PDHK
|
Cancer
|
|
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
|
-
- HY-14660S
-
|
GSK2118436A-d9; GSK2118436-d9
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
|
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
|
-
- HY-124625
-
-
- HY-N2463
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity .
|
-
- HY-137768
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137772
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137769
-
|
3-Mercaptoisobutyric acid
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-W015332
-
|
3-Bromoisobutyric acid
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-W013886
-
|
S-Acetylcaptopril
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity J is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-122661
-
|
MPH
|
PARP
Apoptosis
|
Cancer
|
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .
|
-
- HY-108060
-
-
- HY-108060A
-
|
NM283 dihydrochloride
|
HCV
HCV Protease
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination .
|
-
- HY-145701
-
|
|
MEK
|
Cancer
|
|
MEK1/2-IN-2 is a potent ATP-competitive MEK1/2 inhibitor and shows equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines .
|
-
- HY-130199
-
|
Parellic acid
|
Others
|
Metabolic Disease
|
|
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC50 value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .
|
-
- HY-162107
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-6 (compound 7cc) is an EGCG-like non-competitive inhibitor of DYRK1A. Dyrk1A-IN-6 can be used to alleviate cognitive defects in Down syndrome models .
|
-
- HY-162697
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-69 (compound 5k) is a competitive α-glucosidase inhibitor with an IC50 of 26.8 µM and a Ki value of 26.0 µM. α-Glucosidase-IN-69 has the potential for the diabetes research .
|
-
- HY-113786
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .
|
-
- HY-10079A
-
|
GMX1778 (nicotinate)
|
NAMPT
Apoptosis
|
Cancer
|
|
CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD + and exhibits a potent anticancer activity .
|
-
- HY-128729
-
|
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress .
|
-
- HY-10255AR
-
|
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-10917S
-
|
|
Isotope-Labeled Compounds
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
|
-
- HY-147040
-
|
|
c-Met/HGFR
|
Cancer
|
|
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer .
|
-
- HY-A0166R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (Standard) is the analytical standard of Cilastatin. This product is intended for research and analytical applications. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-17423A
-
|
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-13038A
-
|
R788
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-15141
-
|
Antibiotic AM-2282; STS; AM-2282
|
PKC
PKA
Apoptosis
Bacterial
Fungal
Antibiotic
|
Infection
Cancer
|
|
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 μM. Staurosporine is an apoptosis inducer .
|
-
- HY-B0876
-
|
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-10163S1
-
|
BIBR 953-d3; BIBR 953ZW-d3
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-107597
-
Halicin
1 Publications Verification
SU3327
|
JNK
|
Metabolic Disease
Inflammation/Immunology
|
|
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
|
-
- HY-B1558A
-
|
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease .
|
-
- HY-10163S
-
|
BIBR 953-d4; BIBR 953ZW-d4
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-13966S4
-
|
2-DG-13C-1; 2-Deoxy-D-arabino-hexose-13C-1; D-Arabino-2-deoxyhexose-13C-1
|
Isotope-Labeled Compounds
Apoptosis
Hexokinase
HSV
|
Cancer
|
|
2-Deoxy-D-glucose- 13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
- HY-148757
-
|
|
CaMK
|
Metabolic Disease
|
|
TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively .
|
-
- HY-149515
-
|
|
Monoamine Oxidase
|
Cancer
|
|
MAO-IN-3 (Compound 5) is a reversible and competitive MAO inhibitor (Ki: 0.6 and 0.2 μM for MAO A and MAO B). MAO-IN-3 inhibits LN-229 glioblastoma cell proliferation with an IC50 of 0.8 μM. MAO-IN-3 can be used for cancer research .
|
-
- HY-123206
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea .
|
-
- HY-157068
-
|
|
Ferroptosis
|
Cancer
|
|
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
|
-
- HY-12432R
-
|
|
FLT3
TAM Receptor
|
Cancer
|
|
Gilteritinib (Standard) is the analytical standard of Gilteritinib. This product is intended for research and analytical applications. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
- HY-14660R
-
|
|
Raf
|
Cancer
|
|
Dabrafenib (Standard) is the analytical standard of Dabrafenib. This product is intended for research and analytical applications. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-10336
-
|
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
|
-
- HY-10583
-
|
|
Organoid
ROCK
|
Neurological Disease
Cancer
|
|
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
|
-
- HY-10873
-
|
SU-12662
|
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-14664A
-
-
- HY-15260A
-
|
BMS-863233 monohydrochloride
|
CDK
|
Cancer
|
|
XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
|
-
- HY-19981A
-
|
ARQ-087 Racemate
|
FGFR
|
Cancer
|
|
Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
|
-
- HY-N4193
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
|
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity .
|
-
- HY-N6057
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression .
|
-
- HY-N7377
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment .
|
-
- HY-129993
-
-
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
-
- HY-W010378
-
|
H-D-Asn-OH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Asparagine (H-D-Asn-OH) is a competitive inhibitor of L-Asparagine hydrolysis with a Ki value of 0.24 mM. D-Asparagine is a source of nitrogen for yeast strains. D-Asparagine is a good substrate for the external yeast asparaginase but is a poor substrate for the internal enzyme .
|
-
- HY-P1271
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-115555
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM .
|
-
- HY-138813
-
|
SU-12662 hydrochloride
|
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-134438
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
|
-
- HY-150076
-
|
|
Others
|
Metabolic Disease
Cancer
|
|
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research .
|
-
- HY-151591
-
|
|
Phosphatase
|
Metabolic Disease
|
|
SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
|
-
- HY-148208
-
|
|
Amino Acid Derivatives
|
Metabolic Disease
|
|
S-(p-Nitrobenzyl)glutathione is a competitive glutathionase inhibitor. S-(p-Nitrobenzyl)glutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-(p-Nitrobenzyl)glutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system .
|
-
- HY-160096
-
|
|
ATM/ATR
|
Cancer
|
|
M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities .
|
-
- HY-W371164
-
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
|
-
- HY-N0793R
-
|
|
Cholinesterase (ChE)
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Protopine (Standard) is the analytical standard of Protopine. This product is intended for research and analytical applications. Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
|
-
- HY-118660R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Anhydrotetracycline (hydrochloride) (Standard) is the analytical standard of Anhydrotetracycline (hydrochloride). This product is intended for research and analytical applications. Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells .
|
-
- HY-N7114AR
-
|
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Chloramphenicol succinate (sodium) (Standard) is the analytical standard of Chloramphenicol succinate (sodium). This product is intended for research and analytical applications. Chloramphenicol succinate sodium is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity .
|
-
- HY-15271A
-
|
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM . WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2 . WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively .
|
-
- HY-103353A
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
|
-
- HY-155098
-
|
|
SHP2
|
Cancer
|
|
CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
|
-
- HY-122564
-
|
|
Dynamin
|
Others
|
|
Pyrimidyn 7 is an inhibitor of dynamin I/II with IC50 values of 1.1 μM and 1.8 μM, respectively. Pyrimidyn 7 competitively inhibits the interactions between GTP and phospholipids with dynamin I. Additionally, Pyrimidyn 7 reversibly inhibits clathrin-mediated endocytosis (CME) of transferrin and epidermal growth factor (EGF) in various non-neuronal cell linecell [1.
|
-
- HY-116138
-
|
|
Others
|
Others
|
|
RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.
|
-
- HY-146333
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner .
|
-
- HY-13038
-
|
R788(Disodium)
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-12041
-
|
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis .
|
-
- HY-10044
-
|
WYE-125132
|
mTOR
Apoptosis
|
Cancer
|
|
WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
|
-
- HY-13038B
-
|
R788 disodium hexahydrate
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-15945
-
DBeQ
3 Publications Verification
JRF 12
|
p97
Autophagy
Apoptosis
|
Cancer
|
|
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
|
-
- HY-19928
-
|
EW-7197; TEW-7197
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
|
-
- HY-19928A
-
|
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
|
-
- HY-135111
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-N2554
-
|
Ostenol
|
Monoamine Oxidase
|
Neurological Disease
|
|
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
|
-
- HY-P1380A
-
|
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells .
|
-
- HY-P1178
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-135780A
-
-
- HY-123517
-
|
|
Enterovirus
|
Infection
|
|
DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM .
|
-
- HY-B0876A
-
|
4-Methylpyrazole hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-122936
-
|
|
Histone Methyltransferase
Keap1-Nrf2
Sirtuin
|
Cardiovascular Disease
Cancer
|
|
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
|
-
- HY-10163R
-
|
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (Standard) is the analytical standard of Dabigatran. This product is intended for research and analytical applications. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-B0113
-
|
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0113A
-
|
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-12017
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-10285
-
|
BMS-477118
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-12017A
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 mesylate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 mesylate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-15777
-
|
LEE011
|
CDK
|
Cancer
|
|
RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
|
-
- HY-B0423
-
|
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
- HY-B0549A
-
|
Rec-7-0040; DW61
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-15727
-
|
GSK2110183; LAE002
|
Akt
PKC
ROCK
|
Cancer
|
|
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively .
|
-
- HY-15727A
-
|
GSK2110183 hydrochloride; LAE002 hydrochloride
|
Akt
PKC
ROCK
|
Cancer
|
|
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively .
|
-
- HY-19316
-
|
O6-(Cyclohexylmethyl)guanine
|
CDK
|
Cancer
|
|
NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
|
-
- HY-12866A
-
|
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-15590
-
AZ-23
3 Publications Verification
AZ23; AZ 23
|
Trk Receptor
|
Cancer
|
|
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
|
-
- HY-B0334AS
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam-d5 (sodium) is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].
|
-
- HY-111055
-
|
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect .
|
-
- HY-133117
-
|
|
IKK
|
Cancer
|
|
BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
|
-
- HY-10285A
-
|
BMS-477118 hydrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research .
|
-
- HY-B1729
-
|
|
Oxidative Phosphorylation
Bacterial
|
Infection
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-16448
-
|
BMS-477118 hydrochloride
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research .
|
-
- HY-108657
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
|
-
- HY-15756
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes .
|
-
- HY-15281
-
|
|
mTOR
|
Cancer
|
|
QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
|
-
- HY-115755
-
|
6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5'-triphosphate; 6-Thio-ITP
|
DNA/RNA Synthesis
|
Cancer
|
|
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM) .
|
-
- HY-123419
-
|
|
Histone Demethylase
|
Cancer
|
|
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent .
|
-
- HY-122592
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .
|
-
- HY-120661
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
T-1840383 is a potent, ATP-competitive inhibitor of c-Met/VEGFR-2, with the IC50s of 1.9 nM, 7.7 nM, 2.2 nM and 5.5 nM for c-Met, VEGFR1, VEGFR2 and VEGFR3, respectively .
|
-
- HY-116605
-
|
|
Histone Methyltransferase
|
Cancer
|
|
GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research .
|
-
- HY-136347R
-
|
|
HMG-CoA Reductase (HMGCR)
Drug Metabolite
|
Cardiovascular Disease
|
|
3α-Hydroxy pravastatin (sodium) (Standard) is the analytical standard of 3α-Hydroxy pravastatin (sodium). This product is intended for research and analytical applications. 3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor .
|
-
- HY-19539
-
|
|
Ras
|
Cancer
|
|
NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation .
|
-
- HY-33549
-
|
|
Others
|
Neurological Disease
Cancer
|
|
α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases .
|
-
- HY-B0873R
-
|
|
Cytochrome P450
ROS Kinase
|
Others
|
|
Uniconazole (Standard) is the analytical standard of Uniconazole. This product is intended for research and analytical applications. Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC50 of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a Ki of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent .
|
-
- HY-N7536
-
|
|
TRP Channel
|
Others
|
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
|
-
- HY-10423
-
|
ASP7486
|
mTOR
Autophagy
|
Cancer
|
|
OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively .
|
-
- HY-14664
-
|
XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-17443
-
|
EI546; LY544349; ONO5046
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-17443A
-
|
ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-B0919
-
|
CI-337; O-Diazoacetyl-L-serine; P-165
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Azazerine (CI-337) is a competitive inhibitor of glutamine amidotransferase. Azaserine is an antibiotic, it shows antibacterial activities. Azazerine shows anti-tumor activities and it may also act as a tumor inducer. Azazerine can be used for the research of cancer and infection .
|
-
- HY-16755
-
|
GSK-2586184; GLPG-0778
|
JAK
|
Inflammation/Immunology
|
|
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
|
-
- HY-111388B
-
|
|
CDK
|
Cancer
|
|
SEL120-34A hydrochloride is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-111388
-
|
|
CDK
|
Cancer
|
|
SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-N7433
-
|
Ethylidene-glucose
|
GLUT
Endogenous Metabolite
|
Metabolic Disease
|
|
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport .
|
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
-
- HY-113038B
-
|
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-A0230A
-
|
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure .
|
-
- HY-101964
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively .
|
-
- HY-B0549
-
|
Rec-7-0040 free base; DW61 free base
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-N10489
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-10254G
-
|
PD0325901; PD325901
|
MEK
|
Cancer
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-W099579
-
|
Kojic dipalmitate
|
Tyrosinase
|
Endocrinology
|
|
Kojic acid dipalmitate (Kojic dipalmitate) is a derivative of Kojic acid (HY-W050154), a fungal metabolite that can be produced by species of Aspergillus, Acetobacter and Penicillium. Kojic acid dipalmitate is a slow and reversible competitive inhibitor of tyrosinase. Kojic acid dipalmitate can be used for skin‐lightening agent research .
|
-
- HY-B0418AR
-
|
R-18553 hydrochloride (Standard)
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-138877A
-
|
|
Phosphatase
|
Cancer
|
|
Phosphoglycolic acid (lithium) is a competitive inhibitor of phosphoglycerate mutase (PGAM)-B, an enzyme of the glycolytic pathway. Phosphoglycolic acid increases basal and fMLF-induced levels of G6P in intact neutrophils. Phosphoglycolic acid thereby increases upstream intermediates in neutrophils, thereby amplifying the respiratory oxidative burst .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-163907
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-71 (Compound 7h) is a competitive α-glucosidase inhibitor (IC50: 98.0 µM). α-Glucosidase-IN-71 can be used for research of carbohydrate-related diseases, especially type 2 diabetes mellitus .
|
-
- HY-N6054R
-
|
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-10255R
-
|
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-N12761
-
|
|
Phosphatase
Glucosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A is also an α-glucosidase (α-glucosidase) inhibitor with anti-inflammatory activity .
|
-
- HY-17423R
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir (Standard) is the analytical standard of Abacavir. This product is intended for research and analytical applications. Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-13418A
-
|
Compound C; BML-275
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599) .
|
-
- HY-B0113S
-
|
H 16868-d3
|
Proton Pump
Bacterial
Autophagy
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
|
-
- HY-12481
-
|
|
PI3K
Autophagy
|
Cancer
|
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
|
-
- HY-10195BS
-
|
|
Isotope-Labeled Compounds
PKC
|
Metabolic Disease
|
|
Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
|
-
- HY-15816A
-
|
BVD-523 hydrochloride; VRT752271 hydrochloride
|
ERK
|
Cancer
|
|
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-124817
-
Col003
5 Publications Verification
|
HSP
|
Inflammation/Immunology
|
|
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
|
-
- HY-101523
-
|
|
CDK
|
Cancer
|
|
Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death .
|
-
- HY-16018A
-
|
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
VEGFR
|
Cancer
|
|
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-103442
-
|
DAPH
|
EGFR
Amyloid-β
|
Neurological Disease
Cancer
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
|
-
- HY-16018
-
|
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
|
Cancer
|
|
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-110347
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
|
-
- HY-109184
-
|
AMG 397
|
Bcl-2 Family
|
Cancer
|
|
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer .
|
-
- HY-114038
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research .
|
-
- HY-139409A
-
|
|
Others
|
Metabolic Disease
|
|
2-Deoxy-D-glucose 6-phosphate disodium, a derivative of 2-Deoxy-D-glucose, is produced in mammalian cells by the action of hexokinase on 2-DG. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
|
-
- HY-110313
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research .
|
-
- HY-144354S
-
|
|
Isotope-Labeled Compounds
ASCT
|
Cancer
|
|
S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2[1].
|
-
- HY-151248
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM . HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively .
|
-
- HY-10163S2
-
|
BIBR 953-13C6; BIBR 953ZW-13C6
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
|
-
- HY-149716
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
MEY-003 is an Autotaxin(ATX) inhibitor with EC50s of 460 nM and 1.09 μM for hATX-β and hATX-ɣ (analysis with LPC18:1). MEY-003 behaves as a non-competitive inhibitor with K iof 432 nM. MEY-003 can be used for targeted ATX-related disease research .
|
-
- HY-19101
-
|
|
Kallikrein
|
Cardiovascular Disease
|
|
ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
|
-
- HY-15901A
-
|
|
Pim
mTOR
|
Cancer
|
|
LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-122203A
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-162884
-
|
|
Others
|
Infection
|
|
EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC50 of 2.68 μM and a Ki value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity .
|
-
- HY-B0334R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (Standard) is the analytical standard of Sulbactam. This product is intended for research and analytical applications. Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-12335
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
|
-
- HY-108474
-
|
AG 337
|
Thymidylate Synthase
|
Cancer
|
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
|
-
- HY-111926
-
|
|
Others
|
Metabolic Disease
|
|
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM . N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor .
|
-
- HY-14518
-
|
4-Aminofolic acid; APGA
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-107339
-
|
Harmonyl
|
Angiotensin-converting Enzyme (ACE)
|
Neurological Disease
Metabolic Disease
|
|
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex .
|
-
- HY-133130
-
|
|
MAGL
|
Neurological Disease
|
|
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
|
-
- HY-19826
-
|
|
DNA Methyltransferase
ADC Cytotoxin
Autophagy
Apoptosis
|
Cancer
|
|
Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin .
|
-
- HY-12017B
-
|
|
c-Met/HGFR
|
Cancer
|
|
PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties .
|
-
- HY-P1271A
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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-
- HY-11028
-
|
PF-2413873
|
Progesterone Receptor
|
Endocrinology
|
|
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo .
|
-
- HY-109097
-
|
SP-8203
|
MMP
iGluR
|
Neurological Disease
|
|
Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury .
|
-
- HY-109191
-
|
PHP-201; AMA0076
|
ROCK
|
Others
|
|
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia .
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-
- HY-109191A
-
|
PHP-201 hydrochloride; AMA0076 hydrochloride
|
ROCK
|
Neurological Disease
|
|
Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia .
|
-
- HY-108657A
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
|
-
- HY-148514
-
|
|
PDGFR
|
Cancer
|
|
CT52923 is a selective, orally active platelet-derived growth factor receptor (PDGFR) antagonist. CT52923 also is an ATP-competitive inhibitor. CT52923 can be used for the research variety of pathological diseases, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer .
|
-
- HY-10195A
-
|
LY333531 mesylate
|
PKC
|
Cardiovascular Disease
Metabolic Disease
|
|
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes .
|
-
- HY-100047
-
|
|
Taste Receptor
|
Others
|
|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
-
- HY-161421
-
|
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-61 (Compd 1j), a competitive α-glucosidase inhibitor, demonstrates excellent inhibition with an IC50 of 0.73 μM. α-Glucosidase-IN-61 (Compd 1j) is used for the research of type 2 diabetes mellitus .
|
-
- HY-B0334AR
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (sodium) (Standard) is the analytical standard of Sulbactam (sodium). This product is intended for research and analytical applications. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
|
-
- HY-12853R
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione (Standard) is the analytical standard of Mesotrione. This product is intended for research and analytical applications. Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-162893
-
|
|
Glucosidase
|
Metabolic Disease
|
|
SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
|
-
- HY-148396
-
|
|
DNA/RNA Synthesis
|
Infection
Cancer
|
|
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM .
|
-
- HY-13588
-
|
SCE-129 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
|
-
- HY-B0307A
-
|
5-Iodo-2′-deoxyuridine hydrate; 5-IUdR hydrate; IdUrd hydrate
|
Phosphatase
|
Infection
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) hydrate is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM .
|
-
- HY-108675
-
|
|
MMP
P2X Receptor
|
Infection
Cancer
|
|
PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers .
|
-
- HY-13588B
-
|
SCE-129 sodium hydrate
|
Antibiotic
Bacterial
|
Infection
|
|
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
|
-
- HY-162675
-
|
|
GSK-3
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
COB-187 is a potent, ATP-competitive and selective inhibitor of GSK-3β. COB-187 inhibits GSK-3 through a reversible and Cysteine (Cys)-199-dependent mechanism. COB-187 inhibits LPS induced cytokine production and SARS-CoV-2 spike protein-induced CXCL10 production .
|
-
- HY-N2553
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase .
|
-
- HY-149426
-
|
|
Sirtuin
|
Inflammation/Immunology
|
|
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
|
-
- HY-14721A
-
|
EMD-1214063 hydrochloride
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
|
-
- HY-13011
-
|
CH5424802; RO5424802; RG7853
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-13203
-
|
TAE226
|
FAK
Pyk2
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively .
|
-
- HY-13007
-
|
PF-03758309
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-13024
-
|
DCC-2036
|
Bcr-Abl
FLT3
Src
Apoptosis
|
Cancer
|
|
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
|
-
- HY-15656
-
|
LDK378
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
|
-
- HY-15656A
-
|
LDK378 dihydrochloride
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency .
|
-
- HY-B0236
-
|
EACA; Epsilon-Amino-n-caproic Acid; 6-Aminohexanoic acid
|
Others
|
Metabolic Disease
Cancer
|
|
6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
|
-
- HY-15959
-
|
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
|
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
|
-
- HY-15237
-
|
SL0101
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM . SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM .
|
-
- HY-15847
-
HS38
1 Publications Verification
|
DAPK
|
Cardiovascular Disease
|
|
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders .
|
-
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-13007B
-
|
PF-03758309 dihydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-13007A
-
|
PF-03758309 hydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-117596
-
UNC569
1 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
|
-
- HY-P3229
-
SN52
2 Publications Verification
|
NF-κB
|
Cancer
|
|
SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research .
|
-
- HY-I0096S
-
-
- HY-10163S3
-
|
BIBR 953-13C,d3; BIBR 953ZW-13C,d3
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-A0166S
-
|
MK0791-15N,d3
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
|
-
- HY-B0236A
-
|
EACA hydrochloride; Epsilon-Amino-n-caproic Acid hydrochloride; 6-Aminohexanoic acid hydrochloride
|
Others
|
Metabolic Disease
Cancer
|
|
6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
|
-
- HY-148327
-
|
|
Adenosine Kinase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
AK-IN-1 (compound 4072-2732) is an adenosine kinase (AK) inhibitor that is competitive for adenosine (Ado) but not for ATP. AK-IN-1 inhibits 86%, 87% and 89% of AK activity at concentrations of 2, 4 and 10 µM, respectively. AK-IN-1 has good potential for research in many disease areas, including ischaemia, inflammation and seizures .
|
-
- HY-14721
-
|
EMD-1214063
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
|
-
- HY-159625
-
|
Ro 91-4714
|
PIKfyve
|
Cancer
|
|
WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with Kd values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively. WX8 (Ro 91-4714) inhibits lysosomal fission without effecting homotypic lysosomal fusion. WX8 (Ro 91-4714) is used in the research of autophagy-dependent cancer .
|
-
- HY-P4522
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-10450
-
|
BMS-512148
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-16343C
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (Maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16343
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16343A
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 hydrochloride is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15779
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity .
|
-
- HY-15779A
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .
|
-
- HY-17443B
-
|
EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-B0574S1
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-129944
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-136128
-
|
|
Potassium Channel
|
Cancer
|
|
H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity .
|
-
- HY-111538
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
|
-
- HY-100706
-
|
|
DNA-PK
|
Cancer
|
|
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively .
|
-
- HY-N8122
-
|
|
Akt
|
Cancer
|
|
24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM) .
|
-
- HY-117058
-
|
(6S)-DDATHF
|
Antifolate
|
Cancer
|
|
LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis .
|
-
- HY-10512S
-
-
- HY-113329
-
|
Taurocyamine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats . Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport .
|
-
- HY-W013754
-
|
|
Others
|
Others
|
|
S-Hexylglutathione is an S-substituted glutathione in which the hydrogen of the thiol has been replaced by a hexyl group. S-Hexylglutathione is also an competitive inhibitor against glutathione-S-transferase. S-Hexylglutathione can be used as an affinity chromatographic ligand for glutathione-S-transferase and glutathione peroxidase .
|
-
- HY-113038A
-
|
2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-136990
-
|
|
Others
|
Cancer
|
|
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
|
-
- HY-B0334AS1
-
|
CP45899-d2 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam-d2 (sodium) is the deuterium labeled Sulbactam sodium[1]. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[2][3].
|
-
- HY-156029
-
|
|
Others
|
Cancer
|
|
IA1-8H2 is a non-covalent, non-competitive inhibitor of PHPT1 (IC50: 3.4 μM). IA1-8H2 can be used for research of lung cancer, hepatocarcinoma, and renal cancer .
|
-
- HY-157489
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-47 (compound 8H) is a non-competitive α-glucosidase (α-glucosidase) inhibitor with IC50 value is 38.2 μM and Ki value is 38.2 μM. α-Glucosidase-IN-47 can be used in diabetes research. .
|
-
- HY-B0199AS
-
|
RS 61443-d4 hydrochloride; TM-MMF-d4 hydrochloride
|
Bacterial
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-129808
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
|
-
- HY-134525
-
|
|
iGluR
|
Others
|
|
Ro 8-4304 is a non-competitive, voltage-independent and state-dependent antagonist for NMDA receptor. Ro 8-4304 inhibits 10 μM NMDA-induced currents and 100 μM NMDA-induced currents with IC50s of 2.3 μM and 0.36 μM .
|
-
- HY-100513A
-
|
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
Cancer
|
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 μM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 μM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
|
-
- HY-15586
-
L67
1 Publications Verification
DNA Ligase inhibitor
|
DNA/RNA Synthesis
Caspase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 (DNA Ligase Inhibitor) can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 (DNA Ligase Inhibitor) also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research .
|
-
- HY-155231
-
|
|
Elastase
|
Cancer
|
|
Neutrophil elastase inhibitor 4 (compound 4f) is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM). Neutrophil elastase inhibitor 4 induces T47D cell apoptosis. Neutrophil elastase inhibitor 4 inhibits cell proliferation with IC50s of 21.25, 34.17, 29.93, 99.11 nM for T47D, RPMI 8226, A549, and HSF cells .
|
-
- HY-50878
-
|
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-12067
-
|
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-10249
-
|
|
Akt
AMPK
Autophagy
|
Cancer
|
|
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .
|
-
- HY-12034
-
|
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro .
|
-
- HY-107427
-
|
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
|
-
- HY-107407
-
|
|
Checkpoint Kinase (Chk)
CDK
PKC
Apoptosis
|
Cancer
|
|
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
|
-
- HY-136575
-
|
|
Virus Protease
|
Infection
|
|
4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-136574
-
|
|
Virus Protease
|
Infection
|
|
2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-103274
-
|
|
Bcr-Abl
Src
c-Kit
Apoptosis
|
Neurological Disease
Cancer
|
|
PD180970 is a highly potent and ATP-competitive p210 Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210 Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .
|
-
- HY-141519
-
|
|
Parasite
|
Infection
|
|
PI-55 is a specific cytokinin receptor inhibitor. PI-55 is structurally related to 6-benzylaminopurine (BAP) and was shown to inhibit competitively BAP binding on Arabidopsis-specific receptors CRE1/AHK4 and AHK3. PI-55 inhibits cytokinins induced haustorium formation and increased parasite aggressiveness .
|
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-160687
-
|
|
Others
|
Others
|
|
GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays .
|
-
- HY-W009156R
-
|
|
ATP Citrate Lyase
HIF/HIF Prolyl-Hydroxylase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid (tripotassium hydrate) (Standard) is the analytical standard of Citric acid (tripotassium hydrate). This product is intended for research and analytical applications. Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
|
-
- HY-50867
-
|
CEP-701; KT-5555
|
JAK
FLT3
Trk Receptor
Apoptosis
STAT
|
Cancer
|
|
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
|
-
- HY-153219A
-
|
|
Potassium Channel
|
Endocrinology
|
|
P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .
|
-
- HY-153219
-
|
|
Potassium Channel
|
Endocrinology
|
|
P-CAB agent 2 hydrochloride is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 hydrochloride inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 hydrochloride inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 hydrochloride shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .
|
-
- HY-12866R
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-10262
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity .
|
-
- HY-18086
-
|
SC 204330
|
Pim
|
Cancer
|
|
TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM) .
|
-
- HY-12335A
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
|
-
- HY-103392
-
|
BCX2600
|
Cytochrome P450
|
Neurological Disease
|
|
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
|
-
- HY-101037
-
|
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
|
-
- HY-122629
-
|
|
DAPK
|
Others
|
|
DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively.
DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM) .
|
-
- HY-B0574S2
-
|
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
Mefenamic acid- 13C6 is the 13C-labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-129944A
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-102062
-
|
N-omega-Propyl-L-arginine
|
NO Synthase
|
Neurological Disease
|
|
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS) .
|
-
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-100530B
-
-
- HY-100530C
-
|
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
|
|
Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM .
|
-
- HY-102062A
-
|
N-omega-Propyl-L-arginine hydrochloride
|
NO Synthase
|
Neurological Disease
|
|
Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) hydrochloride is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine hydrochloride displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS) .
|
-
- HY-15141G
-
|
Antibiotic AM-2282; STS; AM-2282
|
PKC
|
Infection
Cancer
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-114203
-
-
- HY-161029
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-122646
-
|
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC50 of 6 nM. USP7-IN-2 causes degradation of MDM2, stabilization of p53 and induction of p21 in multiple cell lines, and can be utilized in cancer research .
|
-
- HY-16638
-
|
PDDF
|
Thymidylate Synthase
|
Metabolic Disease
|
|
CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells .
|
-
- HY-149887
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) (IC50=~10 nM)，which acts function as helicase，ATPase，and exonuclease. WRN exhibits synthetic lethal activity in cancer research. However，H3B-968 inhibits WRN helicase activity，competitively with ATP .
|
-
- HY-10181
-
|
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-13912
-
|
|
Wnt
Porcupine
Casein Kinase
|
Cancer
|
|
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
|
-
- HY-10181A
-
|
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
|
-
- HY-16231
-
|
|
Apoptosis
|
Cancer
|
|
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .
|
-
- HY-122614
-
S29434
2 Publications Verification
NMDPEF
|
Autophagy
|
Neurological Disease
|
|
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
|
-
- HY-107794
-
|
Disodium clodronate tetrahydrate
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
|
-
- HY-D0939
-
|
Chicago Sky Blue 6B
|
Amyloid-β
NF-κB
|
Inflammation/Immunology
|
|
Direct Blue 1 (Chicago Sky Blue 6B) is a complex dye for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1 is a potent and competitive VGLUT inhibitor. Direct Blue 1 can inhibit the Aβ-binding small molecule PrP ligand. Direct Blue 1 has anti-inflammatory activity .
|
-
- HY-118567
-
|
BMOV
|
SHP2
Phosphatase
|
Metabolic Disease
|
|
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer .
|
-
- HY-10181B
-
|
BMS-354825 monohydrate
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib monohydrate also induces apoptosis and autophagy.
|
-
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
-
- HY-110140
-
|
|
CaMK
|
Cardiovascular Disease
Neurological Disease
|
|
(E)-KN-93 phosphate is an inhibitor for Ca 2+/calmodulin-dependent protein kinase II (CaMK II) with IC50 of 9 μM and 3 μM, for CaMKIIδ monomer and CaMKIIδ dodecamer. (E)-KN-93 phosphate binds competitively with Ca 2+/CaM, and disrupts their interaction with CaMK II, and thus inhibits the CaMK II activation .
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-10275
-
|
AR-H067637
|
Thrombin
|
Cardiovascular Disease
|
|
Atecegatran (AR-H067637) is an orally active competitive thrombin inhibitor with a Ki of 2-4 nM. AR-H067637 inhibits platelet activation and aggregation by blocking thrombin binding to fibrin and thrombomodulin. Atecegatran demonstrates significant anticoagulant effects in various plasma coagulation assays, with an IC50 ranging from 93 to 220 nM. Atecegatran can be used in research related to thromboembolic disorders .
|
-
- HY-18637
-
|
|
Deubiquitinase
Apoptosis
|
Neurological Disease
|
|
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
|
-
- HY-15658
-
GSK2801
2 Publications Verification
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .
|
-
- HY-10119
-
|
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-23460
-
|
4-Ethynyl-L-phenylalanine
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B1866
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
|
-
- HY-113468AS
-
|
3-Methoxy-L-tyrosine-d3; 3-O-Methyl-L-DOPA-d3
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
3-O-Methyldopa-d3 is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
|
-
- HY-23460A
-
|
4-Ethynyl-L-phenylalanine hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-137472
-
|
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-137506
-
-
- HY-A0230
-
|
SCH 33844
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure .
|
-
- HY-N1919A
-
|
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-120041
-
|
|
IRAK
|
Cancer
|
|
ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo .
|
-
- HY-N2689
-
|
(R)-6′,7′-DHB
|
Cytochrome P450
|
Cancer
|
|
(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research .
|
-
- HY-N9933
-
|
TβMCA
|
FXR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential .
|
-
- HY-160624
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC50: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer .
|
-
- HY-19010A
-
|
SKF 94482 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 hydrochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 hydrochloride competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-B0574R
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid (Standard) is the analytical standard of Mefenamic acid. This product is intended for research and analytical applications. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-121094
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
|
-
- HY-B0307
-
|
5-Iodo-2′-deoxyuridine; 5-IUdR; IdUrd
|
Phosphatase
Orthopoxvirus
|
Infection
Cancer
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM . Idoxuridine shows anti-orthopoxvirus activity.
|
-
- HY-12830
-
|
|
Pim
|
Cancer
|
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM .
|
-
- HY-136573
-
|
|
Virus Protease
|
Infection
|
|
5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-105184
-
|
|
Cytochrome P450
|
Endocrinology
|
|
YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones .
|
-
- HY-120600
-
|
|
Necroptosis
Apoptosis
RIP kinase
|
Inflammation/Immunology
|
|
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
|
-
- HY-B0113R
-
|
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-10337R
-
|
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β .
|
-
- HY-14281R
-
|
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Standard) is the analytical standard of Trilostane. This product is intended for research and analytical applications. Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-10014
-
R547
2 Publications Verification
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-12062
-
|
|
MEK
|
Cancer
|
|
PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
|
-
- HY-50847
-
|
|
PI3K
Autophagy
|
Cancer
|
|
ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
|
-
- HY-15517
-
KN-92
5 Publications Verification
|
Others
|
Cancer
|
|
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-15517A
-
|
|
Others
|
Cancer
|
|
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-B0488
-
|
L631529; MK401
|
Parasite
|
Infection
|
|
Clorsulon (L631529; MK401) is an orally active flukicidal agent against liver flukes (Fasciola hepatica and Fasciola gigantica) infections in calves and sheep. Clorsulon is also a competitive inhibitor of both 3-phosphoglycorate and ATP andinhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro .
|
-
- HY-13859
-
|
L-FMAU
|
HBV
DNA/RNA Synthesis
Orthopoxvirus
|
Infection
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
|
-
- HY-101870B
-
|
INCB053914 phosphate
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-16214
-
|
LDHA inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts .
|
-
- HY-B0574S
-
|
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively[1][2].
|
-
- HY-13333
-
|
BAG 956
|
PI3K
|
Cancer
|
|
NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
|
-
- HY-10119A
-
|
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-100429
-
CAN508
1 Publications Verification
|
CDK
|
Cancer
|
|
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity .
|
-
- HY-P1297
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect .
|
-
- HY-107365
-
|
|
PI3K
mTOR
|
Cancer
|
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
|
-
- HY-105327
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
|
-
- HY-P2244
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
|
-
- HY-139481
-
|
|
Btk
|
Infection
Cancer
|
|
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively . TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research .
|
-
- HY-101870
-
|
INCB053914
|
Pim
|
Cancer
|
|
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-115741
-
|
|
Others
|
Neurological Disease
Cancer
|
|
3BrB-PP1 is an ATP-competitive analog. 3BrB-PP1 can specifically inhibit the activity of protein kinase with mutations in the ATP-binding pocket (mutation of Thr97 within Sty1’s ATP-binding pocket) .
|
-
- HY-110154
-
|
|
Histone Demethylase
|
Cancer
|
|
NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer .
|
-
- HY-151627
-
-
- HY-N4037
-
|
(-)-Homopterocarpin; 3,9-Dimethoxypterocarpan
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamine oxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress .
|
-
- HY-125221
-
|
|
ROCK
|
Cancer
|
|
DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and induces cell apoptosis. DJ4 can be used for study of cancer .
|
-
- HY-P4522A
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg TFA is a dipeptide. Bz-Ala-Arg TFA is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg TFA can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-111260
-
|
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-107339A
-
|
Harmonyl hydrochloride
|
Angiotensin-converting Enzyme (ACE)
Others
|
Cardiovascular Disease
|
|
Deserpidine hydrochloride (Harmonyl hydrochloride) is an antihypertensive compound that competitively inhibits the activity of angiotensin converting enzyme (ACE). Deserpidine hydrochloride competes with angiotensin I for ACE, preventing the conversion of angiotensin I to angiotensin II, thereby lowering blood pressure. Deserpidine hydrochloride can also reduce angiotensin II-induced aldosterone secretion from the adrenal cortex .
|
-
- HY-B0113S1
-
|
H 16868-d3-1
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-13038AR
-
|
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
|
Fostamatinib (Standard) is the analytical standard of Fostamatinib. This product is intended for research and analytical applications. Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-50683
-
|
|
c-Met/HGFR
|
Metabolic Disease
Cancer
|
|
JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases . JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach .
|
-
- HY-12137
-
|
BI 6727
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-13241
-
|
LY2228820 dimesylate
|
p38 MAPK
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
|
-
- HY-12037A
-
|
ON-01910
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-15816
-
|
BVD-523; VRT752271
|
ERK
|
Cancer
|
|
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-18010
-
|
|
Btk
BCRP
|
Inflammation/Immunology
|
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
|
-
- HY-13011A
-
|
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-W008364
-
|
|
Cytochrome P450
Cannabinoid Receptor
|
Neurological Disease
|
|
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
|
-
- HY-117273
-
|
|
Raf
Autophagy
|
Cancer
|
|
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
|
-
- HY-N0063
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-12137A
-
|
BI 6727 trihydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
|
-
- HY-101368A
-
|
|
Bradykinin Receptor
mAChR
|
Neurological Disease
|
|
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [ 3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [ 3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM) .
|
-
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
|
-
- HY-B0876R
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (Standard) is the analytical standard of Fomepizole. This product is intended for research and analytical applications. Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-161681
-
|
|
Guanylate Cyclase
|
Metabolic Disease
|
|
Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
|
-
- HY-13335
-
|
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε) .
|
-
- HY-16576A
-
SMI-4a
1 Publications Verification
TCS-PIM-1-4a
|
Pim
|
Cancer
|
|
SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .
|
-
- HY-115570
-
|
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
|
-
- HY-117809
-
|
|
PDK-1
|
Cancer
|
|
PDK1-IN-2 is a small molecule inhibitor of 3-phosphoinositol-dependent protein kinase-1 (PDK1). PDK1-IN-2 inhibits the binding of PDK1 to its substrate by competitively binding to the PIF pocket of PDK1, thereby inhibiting the kinase activity and downstream signaling of PDK1. PDK1-IN-2 can be used for cell survival and proliferation in cancer .
|
-
- HY-124953
-
|
|
MAP3K
Apoptosis
|
Cancer
|
|
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities .
|
-
- HY-106103A
-
|
MK 678 acetate; L 36358 acetate
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
|
-
- HY-10229
-
|
AMG 706 Diphosphate
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-13454
-
|
|
PKD
|
Cancer
|
|
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 μM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 μM, respectively). CID 2011756 also has antitumor activity.
|
-
- HY-14722A
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-B0607
-
|
NTBC; Nitisone; SC0735
|
HPPD
|
Metabolic Disease
|
|
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Beta-secretase
|
Neurological Disease
Cancer
|
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-N0192
-
Arbutin
1 Publications Verification
β-Arbutin
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
|
-
- HY-16071
-
AT13148
2 Publications Verification
|
Akt
PKA
ROCK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
|
-
- HY-100125
-
|
SR1368
|
COX
|
Inflammation/Immunology
|
|
Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.
|
-
- HY-17462
-
|
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
|
-
- HY-107526
-
|
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively . NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion .
|
-
- HY-135892
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively .
|
-
- HY-P2244A
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
|
-
- HY-14722C
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-14722
-
|
|
JAK
|
Cancer
|
|
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
|
-
- HY-131760
-
|
2'-Amino-2'-deoxyadenosine-5'-triphosphate, 2′-Amino-2′-deoxy-ATP
|
Others
|
Metabolic Disease
|
|
2'-NH2-ATP (2'-Amino-2'-deoxyadenosine-5'-triphosphate), an adenosine derivative, is a weak competitive inhibitor of ATP, with a Ki of 2.3 mM. 2'-NH2-ATP can be used in nucleic acid labeling .
|
-
- HY-105692
-
|
|
PARP
|
Neurological Disease
|
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo .
|
-
- HY-115750
-
|
|
NO Synthase
|
Neurological Disease
|
|
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
|
-
- HY-100743
-
|
2-Amino-4-phosphonobutyric acid
|
Others
|
Neurological Disease
Metabolic Disease
|
|
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system .
|
-
- HY-150061
-
|
|
PI3K
mTOR
|
Cancer
|
|
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor . NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112346
-
|
|
CDK
Apoptosis
|
Cancer
|
|
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity .
|
-
- HY-110005
-
|
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
Metabolic Disease
|
|
Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM .
|
-
- HY-117359
-
|
|
PAI-1
Apoptosis
|
Cancer
|
|
UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis .
|
-
- HY-P99639
-
|
APL-501; CBT-501; GB-226
|
PD-1/PD-L1
|
Cancer
|
|
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer .
|
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-149528
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Cancer
|
|
MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B (IC50: 1.60 μM). MAO-B-IN-24 also inhibited MAO-A (22.42 μM); at 10 μM concentration, it also reduced AChE and BChE activities to 54.58% and 88.43% .
|
-
- HY-163174
-
|
|
Others
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
II399 is a potent, selective NNMT bisubstrate inhibitor containing an unconventional SAM mimic, with a Ki of 5.9 nM. II399 exhibits an explicit pattern of competitive inhibition for NAM. II399 occupies both the substrate and cofactor binding pockets. II399 has the potential for the research of cancers, metabolic, cardiovascular, and neurodegenerative diseases .
|
-
- HY-134101
-
-
- HY-106103
-
|
MK-678; L-363586
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes .
|
-
- HY-19010
-
|
SKF 94482
|
Histamine Receptor
|
Neurological Disease
|
|
BMY-25368 (SKF 94482) is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food .
|
-
- HY-125625
-
|
|
Renin
|
Cardiovascular Disease
|
|
ES 6864 is an orally active, competitive inhibitor for human renin, with an IC50 of 6.9 nM and a Ki of 7.3 nM. ES 6864 exhibits high species-specific and enzyme-specific properties. ES 6864 exhibits metabolic stability in rat tissue homogenates. ES 6864 reduces blood pressure in rats and sodium-depleted awake marmosets .
|
-
- HY-10583R
-
|
|
ROCK
Organoid
|
Cancer
|
|
Y-27632 (dihydrochloride) (Standard) is the analytical standard of Y-27632 (dihydrochloride). Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
|
-
- HY-15086
-
|
CGS 19755
|
iGluR
|
Neurological Disease
|
|
Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM .
|
-
- HY-168108
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 115 (compound 8n) is a non-competitive chitin synthase (CHS) inhibitor with an IC50 of 93 μM. Antifungal agent 115 demonstrates good selectivity and broad-spectrum antifungal activity, exhibiting significant efficacy against drug-resistant fungi. Antifungal agent 115 can be utilized in fungi infection research .
|
-
- HY-100815
-
|
|
Others
|
Neurological Disease
|
|
(R)-AMPA is an inactive AMPA receptor ligand that inhibits the release of excitatory amino acids from neurons. (R)-AMPA is inactive in experiments that enhance the release of [3H]D-aspartate induced by electrical stimulation. (R)-AMPA is inhibited by competitive and noncompetitive AMPA receptor selective antagonists in response to AMPA and glutamate .
|
-
- HY-18174
-
|
LY2606368
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
|
-
- HY-B0368
-
|
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-18174A
-
|
LY2606368 dihydrochloride
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
|
-
- HY-100201
-
A-196
5 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
|
-
- HY-103265
-
|
FPL 67156 trisodium
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma .
|
-
- HY-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-130250
-
|
|
CDK
Apoptosis
|
Cancer
|
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
|
-
- HY-106934
-
|
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-106634
-
|
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-133120
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- HY-18174B
-
|
LY2606368 Mesylate Hydrate; LY2940930
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
|
-
- HY-106934A
-
|
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-13241A
-
|
LY2228820
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
|
-
- HY-115745
-
|
|
Calmodulin
|
Cardiovascular Disease
|
|
Calmodulin antagonist-1 (A-5) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=66 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=560 μM) in a competitive fashion with respect to cyclic GMP .
|
-
- HY-145597
-
|
|
GLUT
|
Metabolic Disease
Cancer
|
|
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death .
|
-
- HY-18174C
-
|
LY2606368 mesylate
|
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
|
-
- HY-B0368A
-
|
SQ 14225 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril (SQ 14225) hydrochloride, antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-123099
-
|
|
JAK
|
Cancer
|
|
MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling .
|
-
- HY-P0096
-
|
|
Tyrosinase
Sirtuin
|
Inflammation/Immunology
Endocrinology
|
|
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 μM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
|
-
- HY-133120A
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- HY-W011834S
-
|
|
Isotope-Labeled Compounds
HCV
|
Infection
|
|
2'-O-Methylcytidine-d3 is deuterium labeled 2'-O-Methylcytidine (HY-W011834). 2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
|
-
- HY-17423AR
-
|
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir (sulfate) (Standard) is the analytical standard of Abacavir (sulfate). This product is intended for research and analytical applications. Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-120039
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(R)-MDL-101146 is the R-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-120039A
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-18944
-
|
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-N6948S
-
|
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0113S4
-
|
H 16868-d3 sodium
|
Autophagy
Phospholipase
Proton Pump
Bacterial
Isotope-Labeled Compounds
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-118175
-
|
|
Others
|
Others
|
|
RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
|
-
- HY-13588R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cefsulodin (sodium) (Standard) is the analytical standard of Cefsulodin (sodium). This product is intended for research and analytical applications. Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC50 value of 16 μM .
|
-
- HY-11108
-
|
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-W015309
-
|
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-100671
-
|
|
Histone Acetyltransferase
STAT
|
Inflammation/Immunology
Cancer
|
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
|
-
- HY-N1483
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
|
-
- HY-124745
-
|
|
MAP4K
Wnt
Apoptosis
|
Cancer
|
|
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity .
|
-
- HY-131062
-
|
|
Others
|
Metabolic Disease
|
|
yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 µM and a Ki of 1.31 µM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs) .
|
-
- HY-100707
-
|
|
DNA-PK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
|
-
- HY-149300
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research .
|
-
- HY-B0113S3
-
|
H 16868-13C,d3
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-112478
-
|
|
Phosphatase
SHP2
|
Cancer
|
|
PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an 50 of 5.21 μM . PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with 50s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively .
|
-
- HY-120812
-
|
|
HIV Protease
|
Infection
|
|
HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor .
|
-
- HY-N10403
-
|
4-Hydroxy-17β-estradiol
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
|
-
- HY-155137
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
|
Neurological Disease
|
|
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research .
|
-
- HY-10285R
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (Standard) is the analytical standard of Saxagliptin. This product is intended for research and analytical applications. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-14664AR
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (sodium) (Standard) is the analytical standard of Fluvastatin (sodium). This product is intended for research and analytical applications. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-12059
-
AT7867
4 Publications Verification
|
Akt
PKA
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
|
-
- HY-12059A
-
|
|
Akt
PKA
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
|
-
- HY-B0290
-
-
- HY-B1205
-
|
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-10406
-
|
SCIO-469
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-14166
-
|
L 663536
|
FLAP
Leukotriene Receptor
PPAR
Apoptosis
|
Cancer
|
|
MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
|
-
- HY-B0290A
-
|
ONO-1078 hemihydrate
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-18955
-
|
|
MEK
Aurora Kinase
Apoptosis
|
Cancer
|
|
BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10228
-
|
AMG 706
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-13302
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
|
-
- HY-112179
-
|
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .
|
-
- HY-113468AS1
-
|
3-Methoxy-L-tyrosine-d3 hydrate; 3-O-Methyl-L-DOPA-d3 hydrate
|
Isotope-Labeled Compounds
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
|
-
- HY-17395S
-
|
TDT 067-d3 hydrochloride
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-17395AS
-
|
TDT 067-d7
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-101075
-
|
|
Phosphatase
|
Others
|
|
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase .
|
-
- HY-128694
-
|
SR27417
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets .
|
-
- HY-13302B
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
|
-
- HY-133146
-
|
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
|
|
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
|
-
- HY-103195
-
NKY80
1 Publications Verification
|
Adenylate Cyclase
|
Metabolic Disease
|
|
NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
|
-
- HY-100501
-
|
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity .
|
-
- HY-10406A
-
|
SCIO-469 hydrochloride
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
|
-
- HY-116852
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 μM) and competitively binds to tubulin with a Ki of 0.7 μM. Thiocolchicine induces cell apoptosis . Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
|
-
- HY-P1297A
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect .
|
-
- HY-W010342
-
|
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide resultis ATP depletion and synergizes with DNA-crosslinking chemotherapy agents, such as Cisplatin, in killing cancer cells .
|
-
- HY-101075A
-
|
|
Phosphatase
|
Others
|
|
L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase .
|
-
- HY-131350
-
|
|
Proteasome
Parasite
|
Infection
|
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research .
|
-
- HY-112081
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
|
-
- HY-138568
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs) .
|
-
- HY-139466
-
|
|
SHP2
PKC
|
Metabolic Disease
|
|
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases .
|
-
- HY-131592
-
|
|
Apoptosis
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-147298
-
|
CYC140
|
Polo-like Kinase (PLK)
|
Cancer
|
|
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
|
-
- HY-150560
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels .
|
-
- HY-33838
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor 4A3 (eIF4A3) inhibitor. eIF4A3-IN-8 can serve as a valuable chemical probe to elucidate the detailed function of eIF4A3 and EJC (exon junction complex) .
|
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
-
- HY-B1729S
-
|
|
Antibiotic
|
Infection
|
|
Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
|
-
- HY-B1729S1
-
|
|
Bacterial
|
Infection
|
|
Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
|
-
- HY-14166A
-
|
L 663536 sodium salt
|
PPAR
Apoptosis
Leukotriene Receptor
FLAP
|
Cancer
|
|
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis .
|
-
- HY-137321
-
|
Estriol 3-β-D-Glucuronide sodium salt
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Estriol 3-glucuronide (Estriol 3-β-D-Glucuronide) sodium salt is a metabolite of Estriol. Estriol 3-glucuronide sodium salt competitively inhibits the hydrolysis of 4-methylumbelliferyl-β-D-glucuronide (4Mu-GlcU). Estriol 3-glucuronide sodium salt is a substrate for hydrolysis by Klotho-human IgG1 Fc protein (KLFc) .
|
-
- HY-B1729R
-
|
|
Oxidative Phosphorylation
Bacterial
|
Infection
|
|
Phenoxyethanol (Standard) is the analytical standard of Phenoxyethanol. This product is intended for research and analytical applications. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-163433
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC50 value of 0.180 μM and a Ki of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research .
|
-
- HY-134245
-
|
Tubercidin 5'-phosphate; 7-Deaza-AMP
|
Others
|
Others
|
|
7-Deazaadenosine 5'-phosphate (Tubercidin 5'-phosphate; 7-Deaza-AMP) is a potential substrate or competitive inhibitor of enzymes that interact with 5′-adenylic acid monophosphate. As a nucleotide derivative, 7-Deazaadenosine 5'-phosphate can regulate cellular functions by affecting intracellular signaling pathways, especially in signaling involving AMP .
|
-
- HY-B0549AR
-
|
|
Phosphodiesterase (PDE)
Calcium Channel
mAChR
|
Neurological Disease
|
|
Flavoxate (hydrochloride) (Standard) is the analytical standard of Flavoxate (hydrochloride). This product is intended for research and analytical applications. Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections .
|
-
- HY-B0231R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Enalaprilat (dihydrate) (Standard) is the analytical standard of Enalaprilat (dihydrate). This product is intended for research and analytical applications. Enalaprilat dihydrate (MK-422), the active metabolite of the oral proagent Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension .
|
-
- HY-W684904
-
|
|
TGF-β Receptor
|
Cancer
|
|
LY550410 is a small-molecule ATP-competitive inhibitor against type I TGF-β receptor kinase, which contains heteroaryl rings for potent binding to the kinase-domain active site. LY550410 modulates TGF-β signalling, thereby regulates gene expression and ultimately cell growth. LY550410 is promising for research of cancers .
|
-
- HY-162480
-
|
|
Glucosidase
Phosphatase
|
Endocrinology
|
PTP1B-IN-27 (Compound 7i) is an inhibitor of protein tyrosine phosphatase 1-B (PTP‐1B)(IC50=8.2 µM). PTP1B-IN-27 also inhibits α-Glucosidase (IC50=120 µM) and shows competitive inhibition (Ki=118 µM) .
|
-
- HY-14721R
-
|
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
|
-
- HY-12037
-
|
ON-01910 sodium
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-13011S
-
|
CH5424802-d8; RO5424802-d8; AF802-d8
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-110042
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis .
|
-
- HY-13011S1
-
|
CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-157116
-
|
|
ICMT
|
Cancer
|
|
ICMT-IN-48 (compound 1) is an ICMT inhibitor that is competitive (Km=13 μM) for the prenylated methyl acceptor, the first substrate of ICMT. ICMT-IN-48 inhibits ICMT activity with IC50s affected by the concentration of the second substrate S-adenosylmethinine (SAM), and the IC50s are 3.5 μM (1×Km SAM) and 2.3 μM (10×Km SAM), respectively .
|
-
- HY-157382
-
|
|
Cholinesterase (ChE)
Amyloid-β
MMP
|
Neurological Disease
|
|
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
|
-
- HY-114923
-
|
|
DNA-PK
PI3K
|
Cancer
|
|
SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .
|
-
- HY-N4110R
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-123931
-
ZLDI-8
1 Publications Verification
|
Notch
Phosphatase
Apoptosis
|
Cancer
|
|
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM .
|
-
- HY-100434
-
|
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cardiovascular Disease
Cancer
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively . PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor .
|
-
- HY-112291
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-112291A
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-107339R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Neurological Disease
Metabolic Disease
|
|
Deserpidine (Standard) is the analytical standard of Deserpidine. This product is intended for research and analytical applications. Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex .
|
-
- HY-13204AR
-
|
|
mAChR
|
Neurological Disease
|
|
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-12333
-
|
G-749
|
FLT3
Apoptosis
|
Cancer
|
|
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML) .
|
-
- HY-12344
-
UNC2025
4 Publications Verification
|
FLT3
|
Cancer
|
|
UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-12344A
-
|
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-10873S
-
|
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
|
-
- HY-112683
-
|
|
ASCT
|
Cancer
|
|
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
|
-
- HY-112683A
-
|
|
ASCT
|
Cancer
|
|
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
|
-
- HY-136174
-
|
|
PARP
|
Cancer
|
|
RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
|
-
- HY-15491
-
|
|
COX
Apoptosis
|
Cancer
|
|
AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range . AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis .
|
-
- HY-131081
-
|
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin. γ-Amanitin competitively binds to monoclonal antibody (mAb), with an IC50 of 163.1 ng/mL .
|
-
- HY-13302C
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy .
|
-
- HY-10517A
-
|
(Z)-SU6668; (Z)-TSU-68
|
VEGFR
PDGFR
FGFR
|
Cancer
|
|
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors .
|
-
- HY-14892
-
|
LC15-0444
|
Dipeptidyl Peptidase
|
Metabolic Disease
Cancer
|
|
Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-19432
-
|
|
iGluR
|
Neurological Disease
|
|
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 .
|
-
- HY-131800
-
|
|
Others
|
Metabolic Disease
|
|
3'-Deoxy-3'-amino-ATP, an ATP analogue, is a potent and competitive inhibitor of ATP, with a Ki of 2.3 μM. 3'-Deoxy-3'-amino-ATP can be used to synthesis of 3′-Amino-3′-deoxy transfer RNA by incorporation into the 3' terminus of tRNA-C-C .
|
-
- HY-101037S1
-
|
N-Methylglycine-d3; Sarcosin-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
|
-
- HY-144778
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
|
Cancer
|
|
IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
|
-
- HY-13204B
-
|
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-P3678
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
|
-
- HY-148318
-
|
|
Casein Kinase
|
Cancer
|
|
CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies .
|
-
- HY-13418G
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
|
Neurological Disease
Cancer
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-153089
-
|
|
GSK-3
Mitophagy
|
Neurological Disease
|
|
GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA .
|
-
- HY-149248
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-8 competitively antagonizes LPS binding to MD-2. NF-κB-IN-8 reduces the expression of inflammatory factors by binding to MD-2. NF-κB-IN-8 also inhibits ALP activity. NF-κB-IN-8 can be used for the research of inflammation such as acute lung injury (ALI) .
|
-
- HY-W484263
-
|
|
NO Synthase
|
Neurological Disease
|
|
hnNOS-IN-3 (compound 39) is a selective nNOS inhibitor, with a Ki of 0.32 μM. The nNOS binding of hnNOS-IN-3 is competitive with L-arginine. The selectivity of hnNOS-IN-3 for nNOS versus iNOS (Ki=37 μM) and eNOS (Ki=9.4 μM) is 115-fold and 29-fold, respectively .
|
-
- HY-P5038
-
|
c(GRGDSP)
|
Integrin
|
Cancer
|
|
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
|
-
- HY-W758126
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
|
-
- HY-13204R
-
|
KL 373 hydrochloride (Standard)
|
mAChR
|
Neurological Disease
|
|
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
|
-
- HY-158037
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-55 (Compound 8g) is an orally active and competitive alpha-glucosidase inhibitor, with IC50 and Ki values of 12.1 and 9.66 µM, respectively. α-Glucosidase-IN-55 can be used for the research into type 2 diabetes mellitus (T2DM) to improve blood sugar control and metabolic health .
|
-
- HY-10873S2
-
|
SU-12662-d5 hydrochloride
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cancer
|
|
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
|
-
- HY-14518R
-
|
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-10572A
-
|
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
|
|
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
|
-
- HY-U00079A
-
|
FK-176
|
mAChR
|
Neurological Disease
|
|
Vamicamide (FK-176) is an orally active competitive mAChR antagonist that inhibits contractions induced by cholinergic nerve stimulation by preventing mAChR agonists from binding to mAChR. Vamicamide exhibits a good anti-bladder spasm effect, with a pA2 value of 6.82 in bladder tissue. Vamicamide can be used in research within the field of neurological diseases .
|
-
- HY-117583A
-
|
|
HDAC
Histone Methyltransferase
|
Neurological Disease
|
|
BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research .
|
-
- HY-50878R
-
|
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-16569
-
|
|
Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
Cancer
|
|
Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
|
-
- HY-101925
-
CM-272
3 Publications Verification
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
|
-
- HY-15425
-
|
Sphingosine Kinase 1 inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
|
-
- HY-15425B
-
|
Sphingosine Kinase 1 inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
|
-
- HY-113038
-
|
(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling .
|
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-18187
-
|
|
Apoptosis
|
Cancer
|
|
Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
|
-
- HY-123163
-
|
RWJ-66826; RTI-6617-003
|
Progesterone Receptor
Glucocorticoid Receptor
Androgen Receptor
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
|
-
- HY-B0307R
-
|
|
Phosphatase
Orthopoxvirus
|
Infection
Cancer
|
|
Idoxuridine (Standard) is the analytical standard of Idoxuridine. This product is intended for research and analytical applications. Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM . Idoxuridine shows anti-orthopoxvirus activity.
|
-
- HY-116919
-
|
|
Others
|
Cardiovascular Disease
|
|
MLS000536924 is a potent and selective inhibitor of human epithelial 15-lipoxygenase-2 with competitive activity. MLS000536924 exhibits more than 50-fold selectivity in inhibiting h15-LOX-2 and can be effectively applied to study its role in atherosclerosis, cystic fibrosis, and ferroptosis. The binding mode of MLS000536924 shows stronger restriction of protein movement than other inhibitors, further verifying its higher biological activity .
|
-
- HY-13011R
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-15656R
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
IGF-1R
|
Endocrinology
Cancer
|
|
Ceritinib (Standard) is the analytical standard of Ceritinib. This product is intended for research and analytical applications. Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency .
|
-
- HY-10580
-
|
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-P1740A
-
|
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-123872
-
|
|
p97
|
Cancer
|
|
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
|
-
- HY-129997
-
|
|
CD38
NADPH Oxidase
Tyrosinase
|
Cardiovascular Disease
|
|
Luteolinidin chloride is a deoxyanthocyanidin isolated from the plant Sorghum bicolor with antioxidant activity. Luteolinidin chloride is a potent CD38 inhibitor (Ki=11.4 μM) and protects the heart from ischemia/reperfusion injury by preserving endothelial nitric oxide synthase (eNOS) function and preventing endothelial dysfunction. Luteolinidin chloride is also a competitive inhibitor of tyrosinase (IC50=3.7 μM) and blocks the production of melanin .
|
-
- HY-18174E
-
|
LY2606368 dimesylate
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
|
-
- HY-103265B
-
|
FPL 67156 trisodium hydrate
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) trisodium hydrate is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium hydrate is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium hydrate can be used in the research of disease like calcific aortic valve disease, asthma .
|
-
- HY-116815
-
|
|
Beta-lactamase
Bacterial
|
Infection
Neurological Disease
|
|
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
|
-
- HY-103441
-
|
|
EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
|
-
- HY-103265D
-
|
FPL 67156 triethylamine
|
NTPDase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
ARL67156 (FPL 67156) triethylamine is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 triethylamine is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 triethylamine can be used in the research of disease like calcific aortic valve disease, asthma .
|
-
- HY-143288
-
|
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
|
NTPDase-IN-2 (compound 5g) is a selective NTPDase inhibitor with IC50s of 0.04 and 2.27 µM for h-NTPDase-2/-8, respectively. NTPDase-IN-2 non-competitively inhibits h-NTPDase-1/-2 with a Km of 74 µM for h-NTPDase-2. NTPDase-IN-2 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-123983
-
|
|
Pim
DAPK
|
Cardiovascular Disease
|
|
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension .
|
-
- HY-155108
-
|
|
Arginase
|
Cancer
|
|
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
|
-
- HY-124267
-
|
SOMG-833
|
c-Met/HGFR
|
Cancer
|
|
Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
|
-
- HY-145462
-
|
|
Bacterial
|
Infection
|
|
N-cis-octadec-9Z-enoyl-L-Homoserine lactone is a potent inhibitor of AhyI. AhyI (expressing acylhomoserine lactone) is responsible for the biosynthesis of autoinducer-1 (AI-1), commonly referred to as a quorum sensing (QS) signaling molecule, which plays an essential role in bacterial communication. N-cis-octadec-9Z-enoyl-L-Homoserine lactone is a competitive inhibitor of AI-1 biosynthesis .
|
-
- HY-P10552
-
|
|
CXCR
|
Inflammation/Immunology
|
|
pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis .
|
-
- HY-10780
-
|
|
Others
|
Cardiovascular Disease
|
|
JTV-803 mesylate is a human factor Xa inhibitor with oral anticoagulant activity. JTV-803 exhibits competitive inhibition of human factor Xa, with a Ki value of 0.019μM and IC50Value is 0.081μM. JTV-803 is 100 times more selective at inhibiting human factor Xa than its comparator. JTV-803 is an effective oral anticoagulant for the prevention of thrombosis .
|
-
- HY-118061
-
|
|
Others
|
Infection
|
|
VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
|
-
- HY-167920
-
|
S-Sulfoglutathione
|
Others
|
Cancer
|
|
Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
|
-
- HY-103430
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-103430A
-
|
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta . SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation .
|
-
- HY-10450R
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (Standard) is the analytical standard of Dapagliflozin. This product is intended for research and analytical applications. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-10254
-
|
PD0325901; PD325901
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
|
-
- HY-15478
-
WZ811
3 Publications Verification
|
CXCR
|
Endocrinology
Cancer
|
|
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM) .
|
-
- HY-10510
-
|
|
Ribosomal S6 Kinase (RSK)
Autophagy
|
Cancer
|
|
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .
|
-
- HY-B0379A
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-B0394
-
|
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205A
-
|
Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-103392S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Neurological Disease
|
|
Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
|
-
- HY-116000
-
|
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-18263A
-
|
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-18263C
-
|
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-12542
-
|
F 368
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-101037S
-
|
N-Methylglycine-15N; Sarcosin-15N
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
|
-
- HY-N10096
-
|
|
Parasite
|
Infection
|
|
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
|
-
- HY-B0985A
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine has a local anesthetic/analgesic effect. Phenazopyridine is used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine can promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-17504B
-
|
ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-B1205B
-
|
Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
|
-
- HY-50672
-
|
|
Kinesin
Apoptosis
Lipoxygenase
|
Cancer
|
|
MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
|
-
- HY-148595
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
|
-
- HY-155102
-
|
|
PROTACs
Glutaminase
|
Cancer
|
|
PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM. PROTAC TG2 degrader-2 inhibits the cell migration and decreases the level of TG2 in ovarian cancer cells. PROTAC TG2 degrader-2 can be used for ovarian cancer study .
|
-
- HY-155240
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
|
-
- HY-P1173
-
|
Myristoylated L 803; GSK-3β inhibitor XIII
|
GSK-3
Amyloid-β
|
Neurological Disease
|
|
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
|
-
- HY-18263
-
|
SB-656933 hydrochloride
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-17623D
-
|
CJ-12420 Benzoate; RQ-00000004 Benzoate
|
Proton Pump
|
Metabolic Disease
|
|
Tegoprazan Benzoate is the benzoate form of Tegoprazan (HY-17623). Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro .
|
-
- HY-N12688
-
|
|
Glucosidase
Amylases
|
Metabolic Disease
|
|
2,3-Dihydrocalodenin B (Compound 6) is a compound that can be isolated from Knema globularia. 2,3-Dihydrocalodenin B is a potent and non-competitive inhibitor against α-glucosidase and α-amylase, with IC50 values of 1.1 and 2.6 μM, respectively. 2,3-Dihydrocalodenin B can be used for the research of diabetes .
|
-
- HY-111214
-
-
- HY-101258
-
|
|
Parasite
|
Infection
|
|
Cardol triene is a phenol found in cashew nut shell liquid that competitively and irreversibly inhibits mushroom tyrosinase (IC50=22.5 μM). It is schistosomicidal, killing 25, 75, and 100% of S. mansoni worms after 24 hours when used at concentrations of 50, 100, or 200 μM, respectively. It has been used as a starting material for the synthesis of bis-benzoxazines.
|
-
- HY-162738
-
|
|
Cytochrome P450
|
Cancer
|
|
JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704) .
|
-
- HY-W015332R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity D (Standard) is the analytical standard of Captopril EP Impurity D. This product is intended for research and analytical applications. Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-Y0258A
-
|
|
Bacterial
Sodium Channel
|
Neurological Disease
|
|
Benzocaine (hydrochloride) is an orally active local agent that can suppress or relieve pain, that acts on voltage-gated Na + channels at a common receptor, with an IC50 value of 0.8 mM at +30 mV. Additionally, Benzocaine (hydrochloride) non-competitively inhibits Ca-ATPase binding with Ca 2+, with an IC50 of 47.1 mM. Benzocaine (hydrochloride) can be used in research within the field of neuromuscular regulation .
|
-
- HY-101037R
-
|
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (Standard) is the analytical standard of Sarcosine. This product is intended for research and analytical applications. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
|
-
- HY-137768R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity B (Standard) is the analytical standard of Captopril EP Impurity B. This product is intended for research and analytical applications. Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137769R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity C (Standard) is the analytical standard of Captopril EP Impurity C. This product is intended for research and analytical applications. Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-137772R
-
|
|
Drug Metabolite
|
Others
|
|
Captopril EP Impurity E (Standard) is the analytical standard of Captopril EP Impurity E. This product is intended for research and analytical applications. Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-168112
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFR del19 and EGFR del19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .
|
-
- HY-146332
-
|
|
Others
|
Cardiovascular Disease
|
|
Collagen-IN-1 (compound 3), an ortho-carbonyl hydroquinone derivative, is a selective inhibitor on collagen. Collagen-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner with an IC50 value of 1.77 μM. Collagen-IN-1 reduces the expression of P-selectin, activation of glycoprotein IIb/IIIa, and release of adenosine triphosphate and CD63 from platelet. Collagen-IN-1 has the potential for platelet-related thrombosis diseases research .
|
-
- HY-162485
-
|
|
Dengue virus
Virus Protease
|
Infection
|
|
DV-B-120 is a competitive inhibitor for dengue virus (DENV) with IC50s of 5.35, 7.39, 10.49 and 8.58 μM, for DENV-1, DENV-2, DENV-3 and DENV-4, respectively, by inhibiting NS2B-NS3 protease. DV-B-120 exhibits antiviral activity through inhibition of DENV replication .
|
-
- HY-149354
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora Kinases-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora Kinases-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora Kinases-IN-4 can be used for research of triple negative breast cancer (TNBC) .
|
-
- HY-10181R
-
|
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-15893
-
|
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
|
-
- HY-B0442
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442A
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-13531
-
|
|
PI3K
|
Cancer
|
|
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
|
-
- HY-19269
-
|
|
Elastase
|
Inflammation/Immunology
|
|
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
|
-
- HY-103712B
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects .
|
-
- HY-15496
-
|
ER-806201
|
MEK
FLT3
|
Cancer
|
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
- HY-B0236S1
-
|
EACA-d10; Epsilon-Amino-n-caproic Acid-d10; 6-Aminohexanoic acid-d10
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
|
-
- HY-B0236S
-
|
EACA-d6; Epsilon-Amino-n-caproic acid-d6; 6-Aminohexanoic acid-d6
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
|
-
- HY-B0368S
-
|
SQ 14225-d3
|
Isotope-Labeled Compounds
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
|
-
- HY-B0442S
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Endocrinology
|
|
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-B0442C
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-143287
-
|
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
|
NTPDase-IN-1 (compound 5a) is a selective NTPDase inhibitor with IC50s of 0.05, 0.23 and 0.54 µM for h-NTPDase-1/-2/-8, respectively. NTPDase-IN-1 non-competitively inhibits h-NTPDase-1/-2 with a Km of 21 µM for h-NTPDase-1. NTPDase-IN-1 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-13699
-
|
|
GnRH Receptor
PERK
|
Others
|
|
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
|
-
- HY-19989
-
|
L-660711
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
|
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
|
-
- HY-N0063R
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-W008364R
-
|
|
Cytochrome P450
Cannabinoid Receptor
|
Neurological Disease
|
|
Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .
|
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
|
-
- HY-113695
-
|
|
Angiotensin-converting Enzyme (ACE)
Adrenergic Receptor
|
Cardiovascular Disease
|
|
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
|
-
- HY-135111R
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole (Standard) is the analytical standard of 4-Desmethoxy Omeprazole. This product is intended for research and analytical applications. 4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-124131
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
|
-
- HY-112345
-
|
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
|
-
- HY-19674
-
|
SSR182289A free base
|
Thrombin
|
Cardiovascular Disease
|
|
SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
|
-
- HY-10108
-
LY294002
Maximum Cited Publications
769 Publications Verification
|
PI3K
Casein Kinase
DNA-PK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator .
|
-
- HY-15425A
-
|
Sphingosine Kinase 1 inhibitor II Citrate
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
|
-
- HY-100542
-
|
Disodium (R)-2-hydroxyglutarate
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
|
-
- HY-117626
-
|
|
AAK1
Cyclin G-associated Kinase (GAK)
SARS-CoV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
|
-
- HY-105349
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-W015309R
-
|
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-164474
-
|
|
MEK
|
Cancer
|
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-149308
-
|
|
Macrophage migration inhibitory factor (MIF)
|
Infection
|
|
MKA031 (compound 6y) is a non-competitive MIF inhibitor with an IC50 value of 1.7 μM. MKA031 (compound 6y) interferes with MIF/AIF interaction, MIF nuclear translocation, and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced dependent cell death. MKA031 can be used in the study of chronic hepatitis C virus infection .
|
-
- HY-10119R
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-17443BR
-
|
|
Elastase
SARS-CoV
|
Cancer
|
|
Sivelestat (sodium tetrahydrate) (Standard) is the analytical standard of Sivelestat (sodium tetrahydrate). This product is intended for research and analytical applications. Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-17623R
-
|
|
Proton Pump
|
Metabolic Disease
|
|
Tegoprazan (Standard) is the analytical standard of Tegoprazan. This product is intended for research and analytical applications. Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H +/K +-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro .
|
-
- HY-17387
-
|
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-13635A
-
|
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-B0091
-
|
CD271
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-B0091A
-
|
CD 271 sodium salt
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
|
-
- HY-12354
-
|
|
MMP
|
Cancer
|
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity .
|
-
- HY-100414
-
|
BYK61359
|
Proton Pump
|
Metabolic Disease
|
|
Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases .
|
-
- HY-131043
-
|
|
PAK
|
Cancer
|
|
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM) .
|
-
- HY-W008344
-
|
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes .
|
-
- HY-130608
-
|
|
EGFR
|
Cancer
|
|
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
|
-
- HY-W009776
-
|
Suberohydroxamic acid; SBHA
|
HDAC
Apoptosis
|
Cancer
|
|
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively .Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways .Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC) .
|
-
- HY-114209
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM) .
|
-
- HY-17504AS
-
-
- HY-14892A
-
|
LC15-0444 tartrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-138696
-
|
XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
|
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
|
-
- HY-141412
-
|
3-Phospho-D-glyceric acid disodium
|
Enolase
Phosphoglycerate Dehydrogenase (PHGDH)
MDM-2/p53
Apoptosis
|
Infection
|
|
D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalyzed glycolysis process. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase (enolase). D-(-)-3-Phosphoglyceric acid disodium can regulate the activity of phosphoglycerate dehydrogenase (PHGDH) to modulate p53 protein and apoptosis .
|
-
- HY-10583G
-
|
|
ROCK
|
Neurological Disease
Cancer
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-152094
-
|
|
Others
|
Endocrinology
|
|
SRD5A1-IN-1 (Compound 4) is a competitive and covalent steroid 5α-reductase type 1 (SRD5A1) inhibitor with an IC50 of 1.44 µM. SRD5A1-IN-1 modulates SRD5A1 function, leading to a lower level of dihydrotestosterone (DHT) production and SRD5A1 protein suppression .
|
-
- HY-155105
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-14281S
-
|
Win 24540-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
|
-
- HY-120857
-
|
PD 158294
|
Others
|
Others
|
|
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Histamine Receptor
|
Inflammation/Immunology
Cancer
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-129278
-
|
|
Parasite
|
Infection
Cardiovascular Disease
Neurological Disease
|
|
Lunarine is an alkaloid, which can be isolated from the seeds of kale (Lunaria annua). Lunarine lowers the blood pressure, stimulates small intestinal motility, inhibits spontaneous contractions of uterus and nervous system, and exhibits an acute toxicity with LD50 of 62.3 mg/kg in dogs and rabbits. Lunarine exhibits antiparasitic activity through a competitive inhibition of protozoan oxidoreductase trypanothione reductase (TryR) with Ki of 304 μM .
|
-
- HY-B0488R
-
|
|
Parasite
|
Infection
|
|
Clorsulon (Standard) is the analytical standard of Clorsulon. This product is intended for research and analytical applications. Clorsulon (L631529; MK401) is an orally active flukicidal agent against liver flukes (Fasciola hepatica and Fasciola gigantica) infections in calves and sheep.?Clorsulon is also a competitive inhibitor of both 3-phosphoglycorate and ATP andinhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro .
|
-
- HY-B1866R
-
|
|
Androgen Receptor
|
Endocrinology
|
|
Linuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .
|
-
- HY-N1919R
-
|
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-13716
-
|
(S,R)-Noscapine
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-123459
-
|
ABT-232; NS-49; PNO-49B
|
Others
|
Endocrinology
|
|
Garomefrine hydrochlorid (ABT-232) is an α1A-adrenergic agonist with the potential to inhibit urinary incontinence. Garomefrine hydrochlorid showed the greatest contractility in pig nasal mucosal vessels. The biological activity of Garomefrine hydrochlorid has been shown to give it a competitive advantage compared to other drugs. The potency of Garomefrine hydrochlorid makes it a valuable research object in related research .
|
-
- HY-162479
-
|
|
Phosphatase
Amyloid-β
|
Metabolic Disease
|
|
PTP1B-IN-26 (Compound 7a) is a derivative of phenylthiosemicarbazide‐phenoxy‐1,2,3‐triazole‐N‐phenylacetamide. PTP1B-IN-26 is an inhibitor of protein tyrosine phosphatase 1B (PTP-1B). PTP1B-IN-26 is a competitive inhibitor. PTP1B-IN-26 can be used to research in type 2 diabetes .
|
-
- HY-106634R
-
|
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Standard) is the analytical standard of Mitoguazone. This product is intended for research and analytical applications. Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-101676
-
|
NID 525
|
Leukotriene Receptor
PPAR
Cytochrome P450
|
Metabolic Disease
|
|
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
|
-
- HY-N0142
-
|
NSC 407292; RJC 02792
|
SGLT
Endogenous Metabolite
GLUT
|
Metabolic Disease
Cancer
|
|
Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation .
|
-
- HY-12826
-
|
|
Beta-lactamase
Bcl-2 Family
Bacterial
|
Cancer
|
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1) . IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively .
|
-
- HY-N1584
-
|
RU-19110
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-101903
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-101544
-
|
|
FGFR
|
Cancer
|
|
ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .
|
-
- HY-N0376
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
|
-
- HY-N2278
-
|
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications .
|
-
- HY-10032
-
|
PF 00477736
|
Checkpoint Kinase (Chk)
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
|
Cancer
|
|
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
|
-
- HY-101903A
-
|
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-17623
-
|
CJ-12420; RQ-00000004
|
Proton Pump
Potassium Channel
Na+/K+ ATPase
|
Inflammation/Immunology
|
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H +/K +-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H +/K +-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-108907
-
|
|
Casein Kinase
|
Cancer
|
|
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
|
-
- HY-125102
-
|
|
IGF-1R
|
Cancer
|
|
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
|
-
- HY-B0442B
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-162036
-
|
|
Glucosidase
Amylases
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC50 values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC50 values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research .
|
-
- HY-18174H
-
|
LY2606368 lactate
|
Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .
|
-
- HY-137373
-
|
|
PKG
|
Others
|
|
Rp-8-pCPT-cGMPS is a competitive inhibitor of cGMP-dependent protein kinase (PKG) (Ki=0.5 μM). Rp-8-pCPT-cGMPS has high lipid solubility and can more easily penetrate the cell membrane and reach sufficient concentration inside the cell to inhibit cGMP-dependent protein kinase. Rp-8-pCPT-cGMPS can be used to study the activity and function of cGMP-dependent protein kinase in platelets .
|
-
- HY-B0368R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Captopril (Standard) is the analytical standard of Captopril. This product is intended for research and analytical applications. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
|
-
- HY-107794R
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate (disodium tetrahydrate) (Standard) is the analytical standard of Clodronate (disodium tetrahydrate). This product is intended for research and analytical applications. Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl-competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
|
-
- HY-160843
-
|
|
Apoptosis
|
Cancer
|
|
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
|
-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Akt
|
Cancer
|
|
Ipatasertib (GDC-0068) (tosylate) is a highly selective ATP-competitive pan-Akt inhibitor with antitumor effects. Ipatasertib (tosylate) prevents colon cancer growth through p53-independent p53 upregulated modulator of apoptosis (PUMA) dependent Apoptosis. Ipatasertib (tosylate) leads to PUMA activation by inhibiting Akt, thereby activating both FoxO3a and NF-κB synchronously that will directly bind to PUMA promoter, up-regulating PUMA transcription and Bax-mediated intrinsic mitochondrial Apoptosis .
|
-
- HY-N1584C
-
|
RU-19110 lactate
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-10409
-
|
TG-101348; SAR 302503
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-13635
-
|
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is an orally active and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-17504
-
|
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-16903
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-B0985
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-12542A
-
|
Dantrolene sodium hydrate
|
Calcium Channel
Autophagy
|
Others
|
|
Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-107477
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments .
|
-
- HY-15844
-
|
Tyrphostin AG-825
|
EGFR
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity . AG825 significantly accelerates apoptosis of human neutrophils . AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development .
|
-
- HY-108476
-
INDY
2 Publications Verification
|
DYRK
|
Cancer
|
|
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .
|
-
- HY-10409A
-
|
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-14664B
-
|
(3R,5S)-XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-133123
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Cancer
|
|
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors .
|
-
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68?nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
-
- HY-116852S
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
|
-
- HY-B0290S1
-
-
- HY-N0192S
-
|
β-Arbutin-d4
|
Isotope-Labeled Compounds
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
|
-
- HY-12542S
-
|
F 368-13C3
|
Isotope-Labeled Compounds
Glutathione Reductase
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
|
-
- HY-130553
-
|
β-NAAG; β-N-Acetylaspartylglutamic acid
|
Aminopeptidase
mGluR
|
Neurological Disease
|
|
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies .
|
-
- HY-15883
-
|
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
|
-
- HY-152208
-
|
|
SHP2
|
Cancer
|
|
BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC50s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes .
|
-
- HY-113038AS
-
|
2-Hydroxyglutarate-13C5 disodium; 2-Hydroxyglutaric acid-13C5 sodium; 2-Hydroxypentanedioic acid-13C5 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
|
-
- HY-116096
-
|
15(R)-Prostaglandin E1; 15-Epiprostaglandin E1
|
15-PGDH
|
Others
|
|
15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1) is a stereoisomer of PGE1 (HY-B0131) but with less biological activity . 15-epi-PGE1 is a non-competitive inhibitor for human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH) with an IC50 of 170 μM .
|
-
- HY-122489A
-
|
|
Others
|
Cardiovascular Disease
Neurological Disease
|
|
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
|
-
- HY-N0192R
-
|
|
Tyrosinase
Endogenous Metabolite
|
Cancer
|
|
Arbutin (Standard) is the analytical standard of Arbutin. This product is intended for research and analytical applications. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
|
-
- HY-B0607R
-
|
NTBC (Standard); Nitisone (Standard); SC56735 (Standard)
|
HPPD
|
Metabolic Disease
|
|
Nitisinone (Standard) is the analytical standard of Nitisinone. This product is intended for research and analytical applications. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-13404
-
|
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-W011109
-
|
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases .
|
-
- HY-15814
-
|
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
|
-
- HY-13404B
-
|
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404C
-
|
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404A
-
|
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-146142
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
|
-
- HY-146165
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity .
|
-
- HY-B0290R
-
|
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pranlukast (Standard) is the analytical standard of Pranlukast. This product is intended for research and analytical applications. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [ 3H]LTE4, [ 3H]LTD4, and [ 3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
|
-
- HY-11107
-
|
|
c-Met/HGFR
Autophagy
Apoptosis
|
Cancer
|
|
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .
|
-
- HY-10424
-
|
PHA-848125
|
CDK
Autophagy
|
Cancer
|
|
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-10683
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-17395
-
|
TDT 067 hydrochloride
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17395A
-
|
TDT 067
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-19340
-
|
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
|
-
- HY-14664DS
-
|
(3S,5R)-XU 62-320-d6 free acid
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
|
-
- HY-W097792
-
|
5'-O-DMT-dU
|
DNA/RNA Synthesis
|
Others
|
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
|
-
- HY-139467
-
|
|
SHP2
PKC
|
Metabolic Disease
|
|
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats .
|
-
- HY-113038AS1
-
|
2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
|
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
mAChR
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-N11706
-
|
(+)-β-Cedrene
|
Fungal
|
Infection
Inflammation/Immunology
|
|
β-Cedrene ((+)-β-Cedrene) is a sesquiterpene compound that can be isolated from Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibiting antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal activities. β-Cedrene is also a potent competitive inhibitor of the CYP2B6-mediatedbupropion hydroxylase, with a Ki value of 1.6 μM .
|
-
- HY-163457
-
|
|
Aminoacyl-tRNA Synthetase
Parasite
|
Infection
|
|
Antileishmanial agent-27 (compound 7j) is a benzothiazolo-coumarin derivative. Antileishmanial agent-27 is a competitive inhibitor of arginyl-tRNA synthetases (ArgRSs). Antileishmanial agent-27 shows selectivity toward ArgRS of Leishmania donovani (LdArgRS) than its human counterpart (HsArgRS), with IC50 values of 1.2 and 19 μM, respectively. Antileishmanial agent-27 possesses high pharmacokinetic properties .
|
-
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
-
- HY-123480
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
EGIS-7625 is a selective and competitive 5-HT2B inhibitor with pKi values of 9.0, 6.2, 7.7 for 5-HT2B, 5-HT2A, 5-HT2C, respective. EGIS-7625 partially attenuates m-chlorophenylpiperazine-induced hypomotility and hypophagia .
|
-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-19989A
-
|
L-660711 sodium
|
Leukotriene Receptor
LPL Receptor
|
Inflammation/Immunology
|
|
MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
|
-
- HY-100034
-
|
DA-3003-1
|
Phosphatase
Histone Methyltransferase
|
Cancer
|
|
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
|
-
- HY-N1584A
-
|
RU-19110 hydrobromide
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-17499
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .
|
-
- HY-N1584B
-
|
RU-19110 hydrochloride
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
|
-
- HY-162642
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bfl-1-IN-3 (Compound 56) is a selective, competitive inhibitor for Bfl-1 on BID binding site with Ki of 105 nM. Bfl-1-IN-3 inhibits the proliferation of cell pfeiffer and MV4-11, with IC50 of 6.92 μM and 12.6 μM. Bfl-1-IN-3 induces apoptosis in pfeiffer cells. Bfl-1-IN-3 overcomes Venetoclax (HY-15531) resistance at the cellular level, and shows synergistically enhanced anti-tumor activity with Venetoclax .
|
-
- HY-155108B
-
|
|
Arginase
|
Cancer
|
|
OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
|
-
- HY-135680
-
|
I-OMe-AG 538
|
IGF-1R
|
Metabolic Disease
Cancer
|
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM .
|
-
- HY-50878AS
-
|
PF-02341066-d9 hydrochloride
|
c-Met/HGFR
Autophagy
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Isotope-Labeled Compounds
|
Cancer
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-16569R
-
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Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
Cancer
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Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
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-
- HY-118084
-
|
Tyrene CR-4
|
JAK
Bcr-Abl
FLT3
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
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|
LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies .
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-
- HY-164685
-
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Phosphodiesterase (PDE)
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Neurological Disease
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|
T-0156 free base is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 free base specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 free base inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 free base enhances the nitric oxide (NO)/cGMP pathway .
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-
- HY-10524
-
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IGF-1R
Insulin Receptor
Apoptosis
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Endocrinology
Cancer
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|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity .
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-
- HY-120214
-
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Syk
RET
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Inflammation/Immunology
|
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TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases .
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- HY-16749A
-
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PLX-3397 hydrochloride
|
c-Fms
c-Kit
Apoptosis
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Cancer
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Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity .
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- HY-N0241
-
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Cholinesterase (ChE)
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Metabolic Disease
|
|
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
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- HY-W011266
-
|
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PDGFR
|
Cancer
|
|
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
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- HY-14664CS
-
|
(3S,5R)-XU 62-320-d6
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
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-
- HY-125957
-
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PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM) and myosin light chain kinase (MLCK) (Ki=7.4 μM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively .
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-
- HY-P3143
-
|
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PD-1/PD-L1
|
Cancer
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|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50?of 7.68?nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST?and SPR assays, respectively.?BMSpep-57?facilitates T cell function by in creasing IL-2 production in PBMCs .
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- HY-139577
-
|
IMB-1018972; IMB-101
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat (IMB-1018972) is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat can be used for research on cardiovascular diseases .
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- HY-W401531S
-
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|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
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- HY-W401531S1
-
|
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Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-O-Methyldopa-d3 (hydrochloride) is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
|
-
- HY-117583
-
|
|
HDAC
Histone Methyltransferase
|
Neurological Disease
|
|
cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. cis-BG47 can be used for neurological disease research .
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- HY-76474A
-
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Apoptosis
Syk
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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-
- HY-N12109
-
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Others
|
Others
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Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
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-
- HY-162390
-
|
|
Amylases
Glucosidase
|
Endocrinology
|
|
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .
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-
- HY-76474
-
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|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
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|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
- HY-13260
-
|
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
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-
- HY-13285
-
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Debio 0719
|
LPL Receptor
|
Neurological Disease
Cancer
|
|
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK . Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells .
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-
- HY-16993
-
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Histone Methyltransferase
Apoptosis
|
Cancer
|
|
OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
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- HY-B0091S
-
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RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
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-
- HY-114263
-
NXT629
3 Publications Verification
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
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-
- HY-101283
-
HCH6-1
3 Publications Verification
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases .
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-
- HY-101193
-
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Zn(II)-protoporphyrin IX; ZnPP; Zinc Protoporphyrin-9
|
Reactive Oxygen Species
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
|
-
- HY-14664C
-
|
(3S,5R)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-117026
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-124828
-
|
|
HuR
|
Cancer
|
|
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation .
|
-
- HY-119366
-
|
|
ROR
|
Inflammation/Immunology
|
|
S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations .
|
-
- HY-119016
-
SK1-I
1 Publications Verification
BML-258
|
SphK
|
Cancer
|
|
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .
|
-
- HY-119016A
-
|
BML-258 hydrochloride
|
SphK
|
Cancer
|
|
SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .
|
-
- HY-100813
-
|
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats .
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-
- HY-144636
-
|
|
Atg4
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
|
-
- HY-W107464
-
G6PDi-1
2 Publications Verification
|
PDI
|
Metabolic Disease
Inflammation/Immunology
|
|
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
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-
- HY-13635S
-
|
MK-906-d9
|
Isotope-Labeled Compounds
5 alpha Reductase
|
Cancer
|
|
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
|
-
- HY-17395B
-
|
TDT 067 lactate
|
Antibiotic
Fungal
Bacterial
|
Infection
|
|
Terbinafine lactate (TDT 067 lactate) is an orally active and potent antifungal agent. Terbinafine lactate is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine lactate also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine (lactate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-B1324A
-
|
Ro 13-8996 free base
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
-
- HY-13635R
-
|
MK-906 (Standard)
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-B0091R
-
|
CD271 (Standard)
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Adapalene (Standard) is the analytical standard of Adapalene. This product is intended for research and analytical applications. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-B0379AR
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-B1205AR
-
|
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-12542R
-
|
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
Dantrolene (Standard) is the analytical standard of Dantrolene. This product is intended for research and analytical applications. Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-B0394R
-
|
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-402410
-
|
|
TET Protein
|
Cancer
|
|
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research .
|
-
- HY-117053
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ 3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ 3H]NKA to cloned human NK-2R .
|
-
- HY-13716R
-
|
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
|
-
- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
|
-
- HY-133028
-
|
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases .
|
-
- HY-157404
-
|
|
Pim
|
Cancer
|
|
Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
|
-
- HY-B0442R
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-11009
-
|
|
CDK
PKC
|
Cancer
|
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
|
-
- HY-10256
-
|
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-18299
-
|
NG 95
|
CDK
Parasite
|
Infection
Cancer
|
|
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
|
-
- HY-10256A
-
|
SB 203580 hydrochloride; RWJ 64809 hydrochloride
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-B0385
-
|
FOY
|
Proteasome
Factor Xa
|
Inflammation/Immunology
|
|
Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
|
-
- HY-108601A
-
|
|
PKC
|
Neurological Disease
Inflammation/Immunology
|
|
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
|
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
|
-
- HY-160250
-
|
|
UGT
|
Metabolic Disease
|
|
UGT1A1-IN-1 (compound 2) is a non-competitive inhibitor of UGT1A1, which can inhibit the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. UGT1A1-IN-1 (compound 2) can bind on UGT1A1 at the same ligand-binding site as bilirubin (HY-N0323). UGT1A1-IN-1 can serve as a ‘turn-on’ fluorescent probe substrate for UGT1A1 .
|
-
- HY-160478
-
|
|
Bcr-Abl
|
Cancer
|
|
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
|
-
- HY-110196
-
|
|
Others
|
Others
|
|
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
|
-
- HY-B0442AS
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-14243
-
|
|
Anaplastic lymphoma kinase (ALK)
Insulin Receptor
VEGFR
Tie
|
Cancer
|
|
CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma .
|
-
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
|
-
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
|
-
- HY-111388A
-
|
|
CDK
|
Cancer
|
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 . Has anti-tumor activity .
|
-
- HY-13404R
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-N0226
-
|
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-121638A
-
|
|
Apoptosis
DGK
|
Cancer
|
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-107522
-
|
|
EAAT
|
Neurological Disease
|
|
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-110137A
-
|
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
|
-
- HY-W011428
-
|
|
CDK
|
Others
Cancer
|
|
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
|
-
- HY-110137
-
|
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
|
-
- HY-N0142R
-
|
NSC 407292 (Standard); RJC 02792 (Standard)
|
SGLT
Endogenous Metabolite
GLUT
|
Metabolic Disease
Cancer
|
|
Phloretin (Standard) is the analytical standard of Phloretin. This product is intended for research and analytical applications. Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA)?and allergic airway inflammation .
|
-
- HY-120826
-
|
|
Monoamine Oxidase
Adenosine Receptor
|
Neurological Disease
|
|
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
|
-
- HY-B0442BR
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-N1584BR
-
|
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects [4] .
|
-
- HY-12542AR
-
|
|
Calcium Channel
Autophagy
|
Others
|
|
Dantrolene (sodium hemiheptahydrate) (Standard) is the analytical standard of Dantrolene (sodium hemiheptahydrate). This product is intended for research and analytical applications. Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-17395AR
-
|
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine (Standard) is the analytical standard of Terbinafine. This product is intended for research and analytical applications. Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17395R
-
|
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Terbinafine hydrochloride (Standard) is the analytical standard of Terbinafine hydrochloride. This product is intended for research and analytical applications. Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17504A
-
|
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-N0235
-
|
(S)-(+)-Bakuchiol
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-16749
-
|
PLX-3397
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity .
|
-
- HY-B1324
-
|
Ro 13-8996
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-107691
-
|
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
|
-
- HY-104066
-
|
Xiliertinib; HMPL-309
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-113914
-
|
Elraglusib
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
|
9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents .
|
-
- HY-100195
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
|
-
- HY-A0009S
-
|
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-104066A
-
|
Xiliertinib tartrate; HMPL-309 tartrate
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P4160
-
|
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
-
- HY-139577A
-
|
MB-1018972 trihydrochloride; IMB-101 trihydrochloride
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat trihydrochloride (IMB-1018972 trihydrochloride) is the trihydrochloride salt form of Ninerafaxstat (HY-139577). Ninerafaxstat trihydrochloride is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat trihydrochloride can be used for research on cardiovascular diseases .
|
-
- HY-17504R
-
|
Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-153896
-
|
|
c-Met/HGFR
|
Cancer
|
|
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
|
-
- HY-14664F
-
|
(3R,5S)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cancer
|
|
(3R,5S)-Fluvastatin ((3R,5S)-XU 62-320) sodium is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-155280
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-60 (compound 5a) is an S-adenosylmethionine (SAM)-competitive and irreversible SARS-CoV-2 nsp16-nsp10 methyltransferase activity inhibitor with an IC50 of 9 μM and a Ki of 26 μM. SARS-CoV-2-IN-60 can specifically occupy a newly identified pocket adjacent to the SAM-binding site on nsp16. SARS-CoV-2-IN-60 has the potential for pan-coronavirus therapeutics .
|
-
- HY-116143
-
|
|
MAGL
|
Metabolic Disease
|
|
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis .
|
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-17504BS2
-
|
ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
|
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17387S1
-
|
Huperzine A-d4
|
iGluR
Cholinesterase (ChE)
Apoptosis
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-B0985R
-
|
|
TRP Channel
|
Neurological Disease
|
|
Phenazopyridine (hydrochloride) (Standard) is the analytical standard of Phenazopyridine (hydrochloride). This product is intended for research and analytical applications. Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases .
|
-
- HY-130337
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Teicoplanin A2-2 is a glycopeptide antibiotic. Teicoplanin A2-2 exhibits antibacterial activity, particularly against coagulase-negative staphylococci (CNS). Teicoplanin A2-2 inhibits bacterial cell wall synthesis by competitively binding to the terminal D-Ala-D-Ala peptide bonds in the cell wall synthesis process, leading to bacterial death. Teicoplanin A2-2 can be used for research into bacterial resistance mechanisms and the development of new antibiotics .
|
-
- HY-13716S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Opioid Receptor
|
Cancer
|
|
Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-119013
-
|
|
Others
|
Cardiovascular Disease
|
|
VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors. The activity of VPC32183 can inhibit lipid phosphatase 1 (LPP1), thereby preventing the activation of ERK(1/2) by dioctanoic acid diglyceride (DGPP 8:0). By reducing the expression of LPP1, VPC32183 can further reduce DGPP 8:0-induced ERK(1/2) activation. The effects of VPC32183 suggest that it may have a positive regulatory function in cell signaling processes .
|
-
- HY-N0226A
-
|
|
Cholinesterase (ChE)
Beta-secretase
Reactive Oxygen Species
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
|
-
- HY-12215
-
|
PF-06463922
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-129636
-
|
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-121744
-
PS10
2 Publications Verification
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
|
-
- HY-107522B
-
|
|
EAAT
|
Neurological Disease
|
|
DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
|
-
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-155141
-
|
|
Cytochrome P450
|
Cancer
|
|
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
|
-
- HY-108601
-
|
|
PKC
|
Inflammation/Immunology
|
|
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
|
-
- HY-N1584AR
-
|
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrobromide) (Standard) is the analytical standard of Halofuginone (hydrobromide). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-121998
-
|
|
Aurora Kinase
|
Others
|
|
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
|
-
- HY-135509
-
|
PF-06463922 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-163879
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
|
-
- HY-B0385R
-
|
|
Proteasome
Factor Xa
|
Inflammation/Immunology
|
|
Gabexate (mesylate) (Standard) is the analytical standard of Gabexate (mesylate). This product is intended for research and analytical applications. Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-10450A
-
|
BMS-512148 (2S)-1,2-propanediol, hydrate
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-12214A
-
|
|
CDK
Apoptosis
|
Cancer
|
|
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
|
-
- HY-17504D
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504C
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-151453
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
|
-
- HY-17623S
-
|
CJ-12420-d6; RQ-00000004-d6
|
Proton Pump
Na+/K+ ATPase
|
Metabolic Disease
|
|
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
MARCKS
PKA
PKC
|
Others
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
-
- HY-122595
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
|
-
- HY-117747
-
|
JCR 424; XM 323
|
HIV Protease
|
Infection
|
|
DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
|
-
- HY-19633A
-
|
|
Others
|
Neurological Disease
|
|
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
|
-
- HY-N2071
-
Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
- HY-146691
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10071
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-15346
-
|
BAY 80-6946
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-B0267A
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-11010
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
- HY-17422S1
-
|
Aciclovir-d4; Acycloguanosine-d4
|
Isotope-Labeled Compounds
HSV
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
|
-
- HY-N6789
-
KT5720
3 Publications Verification
|
PKA
|
Neurological Disease
Cancer
|
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
|
-
- HY-15346A
-
|
BAY 80-6946 dihydrochloride
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
|
-
- HY-125959
-
Ucf-101
1 Publications Verification
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect .
|
-
- HY-W324243
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment .
|
-
- HY-149880
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10071A
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-11010A
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 TFA is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 TFA exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
- HY-12215R
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-121638
-
|
|
Apoptosis
DGK
|
Inflammation/Immunology
Cancer
|
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-N5072
-
|
4',6,7-Trihydroxyisoflavone
|
CDK
PI3K
PKC
|
Cancer
|
|
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.
Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
|
-
- HY-141635
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
cis-11,14-Eicosadienoic acid methyl ester is a more lipid soluble form of the ω-6 C20-2 fatty acid 11(Z),14(Z)-eicosadienoic acid, a naturally occurring PUFA. 11(Z),14(Z)-Eicosadienoic acid competitively inhibits inosine 5’-monophosphate dehydrogenase (Ki=3.1 μM) and inhibits the binding of LTB4 to its receptor on neutrophils (Ki=3.0 μM). Also, serum levels of eicosadienoic acids negatively correlate with degree of sleep disturbance.3 Eicosadienoic acids are converted by desaturases, in vivo, to eicosatrienoic acids, which are potent vasodilators.
|
-
- HY-N1957
-
|
γ-Mangostin
|
5-HT Receptor
COX
Transthyretin (TTR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
- HY-101193S
-
|
Zn(II)-protoporphyrin IX-d2,15N2; ZnPP-d2,15N2; Zinc Protoporphyrin-9-d2,15N2
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
|
-
- HY-B1324R
-
|
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
Cancer
|
|
Oxiconazole nitrate (Standard) is the analytical standard of Oxiconazole nitrate. This product is intended for research and analytical applications. Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
|
-
- HY-N0235R
-
|
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-12583
-
A-366
3 Publications Verification
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
|
-
- HY-120877
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively . MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-108548
-
|
Rp-8-Bromo-PET-cGMPS
|
Others
|
Inflammation/Immunology
|
|
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
|
-
- HY-N2071R
-
|
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
- HY-123597
-
|
DDUG; NCI C04808
|
Others
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
|
-
- HY-112457
-
|
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2 .
|
-
- HY-101308
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
|
-
- HY-101308A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
|
-
- HY-149008
-
|
|
Amylases
|
Metabolic Disease
Cancer
|
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
|
-
- HY-116973
-
|
|
HIV
|
Infection
|
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
|
-
- HY-164393
-
|
|
JAK
Bcr-Abl
Apoptosis
|
Cancer
|
|
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
|
-
- HY-B1311
-
|
SKF-525A; U-5446; RP-5171
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
|
-
- HY-120877A
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-15346R
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-137191
-
|
|
EGFR
|
Cancer
|
|
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
|
-
- HY-B0267AR
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin (chloride) (Standard) is the analytical standard of Oxybutynin (chloride). This product is intended for research and analytical applications. Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB) . Oxybutynin (chloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N1957R
-
|
|
5-HT Receptor
COX
Transthyretin (TTR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
- HY-136265
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
|
-
- HY-161449
-
|
|
11β-HSD
|
Metabolic Disease
|
|
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
|
-
- HY-19261
-
|
|
Others
|
Metabolic Disease
|
|
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
|
-
- HY-B1311R
-
|
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
|
-
- HY-145836
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
|
-
- HY-10450AR
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) (Standard) is the analytical standard of Dapagliflozin ((2S)-1,2-propanediol, hydrate). This product is intended for research and analytical applications. Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-117811
-
|
L-680574
|
Others
|
Others
|
|
(R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guinea pigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
|
-
-
-
HY-L158
-
|
|
4,918 compounds
|
|
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4,918 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0145
-
|
Resorufin ethyl ether
|
Chromogenic Substrates
|
|
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
|
-
- HY-D0939
-
|
Chicago Sky Blue 6B
|
Dyes
|
|
Direct Blue 1 (Chicago Sky Blue 6B) is a complex dye for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1 is a potent and competitive VGLUT inhibitor. Direct Blue 1 can inhibit the Aβ-binding small molecule PrP ligand. Direct Blue 1 has anti-inflammatory activity .
|
-
- HY-10583G
-
|
|
Fluorescent Dye
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-D1493
-
|
|
Fluorescent Dyes/Probes
|
|
FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .
|
-
- HY-10254G
-
|
PD0325901 (GMP); PD325901 (GMP)
|
Fluorescent Dye
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-15141G
-
|
Antibiotic AM-2282 (GMP); STS (GMP); AM-2282 (GMP)
|
Fluorescent Dye
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-13418G
-
|
Compound C dihydrochloride (GMP); BML-275 dihydrochloride (GMP)
|
Fluorescent Dye
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Fluorescent Dye
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
| Cat. No. |
Product Name |
Type |
-
- HY-126388
-
|
|
Enzyme Substrates
|
|
Trypsin Inhibitor, soybean is a potent and reversible inhibitor of trypsin .
|
-
- HY-126306
-
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Biochemical Assay Reagents
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-B1295
-
|
Litarex tetrahydrate
|
Biochemical Assay Reagents
|
|
Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects .
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Biochemical Assay Reagents
|
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-118563
-
|
|
Biochemical Assay Reagents
|
|
S-Farnesyl thioacetic acid is an analog of S-farnesyl cysteine, which is a prenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase) competitive inhibitors. It also inhibits the methylation of farnesylated and geranylgeranylated substrates.
|
-
- HY-W039920
-
|
β-D-Galactosylamine, 98%
|
Carbohydrates
|
|
1-Amino-1-deoxy-β-D-galactose, 98% is a galactose analog used as a competitive inhibitor to aid in the separation, purification, identification, differentiation, and characterization of β-D-galactosidase and galactose oxidase.
|
-
- HY-134438
-
|
|
Enzyme Substrates
|
|
Hexanoyl coenzyme A trilithium is a hexanoyl-based medium-chain fatty acyl coenzyme A that is present in all organisms. Hexanoyl coenzyme A trilithium can be used as a precursor for cannabinoid biosynthesis and acts as a competitive inhibitor of medium-chain acyl coenzyme A dehydrogenase (MCAD) .
|
-
- HY-10254G
-
|
PD0325901 (GMP); PD325901 (GMP)
|
Biochemical Assay Reagents
|
|
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor .
|
-
- HY-15141G
-
|
Antibiotic AM-2282 (GMP); STS (GMP); AM-2282 (GMP)
|
Biochemical Assay Reagents
|
|
Staurosporine (AM-2282) (GMP) is Staurosporine (HY-15141) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases .
|
-
- HY-13418G
-
|
Compound C dihydrochloride (GMP); BML-275 dihydrochloride (GMP)
|
Biochemical Assay Reagents
|
|
Dorsomorphin dihydrochloride (GMP) is the GMP level of Dorsomorphin dihydrochloride (HY-13418). GMP guidelines are used to produce Dorsomorphin dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Dorsomorphin dihydrochloride (GMP) is a potent, selective and ATP-competitive AMPK inhibitor. Dorsomorphin dihydrochloride (GMP) can be used for the research of induced differentiation of pluripotent stem cells (PSCs) .
|
-
- HY-10583G
-
|
|
Biochemical Assay Reagents
|
|
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Biochemical Assay Reagents
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-W097792
-
|
5'-O-DMT-dU
|
Gene Sequencing and Synthesis
|
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1292
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-P2271
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-W013407
-
|
|
Peptides
|
Neurological Disease
|
|
α-Methyltyrosine methyl ester hydrochloride is a competitive tyrosine hydroxylase inhibitor that inhibits the conversion of tyrosine to dopamine. α-Methyltyrosine methyl ester hydrochloride can be used as a tool for sympathetic nervous system research .
|
-
- HY-P2333A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
LCKLSL hydrochloride is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL hydrochloride potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL hydrochloride also inhibits the generation of plasmin and has anti-angiogenic roles .
|
-
- HY-P1292A
-
|
|
PKG
|
Cancer
|
|
PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM .
|
-
- HY-P4543
-
-
- HY-P1315
-
|
Glycylglycyl-L-tyrosyl-L-arginine
|
Cathepsin
|
Others
|
|
Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2 .
|
-
- HY-P10657
-
-
- HY-P3786
-
|
|
PKA
PKC
|
Cancer
|
|
H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
|
-
- HY-P2333
-
|
|
Peptides
|
Cardiovascular Disease
|
|
LCKLSL is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL also inhibits the generation of plasmin and has anti-angiogenic roles .
|
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-P4633
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet .
|
-
- HY-P10346
-
|
Smooth-Muscle Myosin Light-Chain Kinase (796-815)
|
Peptides
|
Cardiovascular Disease
Inflammation/Immunology
|
|
smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction .
|
-
- HY-P2477
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1 .
|
-
- HY-13634B
-
-
- HY-P0222
-
|
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P4270
-
|
|
Peptides
|
Neurological Disease
|
|
Met-Arg-Phe-Ala is a peptide. Met-Arg-Phe-Ala also is a potent competitive inhibitor for enkephalin-generating endopeptidase (EGE). Met-Arg-Phe-Ala can be used for the research of neurological disease .
|
-
- HY-111173
-
|
|
Dipeptidyl Peptidase
|
Others
|
|
Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
|
-
- HY-P0222A
-
|
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P0322
-
|
EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
-
- HY-P1271
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-P1380A
-
|
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells .
|
-
- HY-P1178
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-P1293
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-P1271A
-
|
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-W142169
-
|
Formyl-L-histidine
|
Peptides
|
Others
|
|
N-Formyl-L-histidine shows binding affinity to histidyl-tRNA synthetase with a Ki value of 4.6 μM. N-Formyl-L-histidine shows a competitive inhibition against L-histidine ammonia-lyase, inhibits urocanic acid formation from L-histidine with a Ki value of 4.26 mM .
|
-
- HY-100047
-
|
|
Taste Receptor
|
Others
|
|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
-
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-P3229
-
SN52
2 Publications Verification
|
NF-κB
|
Cancer
|
|
SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research .
|
-
- HY-P5950
-
|
Adrenocorticotropic hormone (6-24)
|
Peptides
|
Cardiovascular Disease
|
|
ACTH (6-24) (human) (Adrenocorticotropic hormone (6-24)) is an ACTH fragment. ACTH (6-24) (human) is a competitive inhibitor of steroidogenesis induced by ACTH (1-39) and ACTH (5-24) (Kd:13.4 and 3.4 nM). ACTH (6-24) (human) inhibits corticosterone production and cAMP accumulation induced by hPTH 1-34 .
|
-
- HY-P4522
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-P1293A
-
|
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-P3248
-
|
Myelin basic protein (85-99) antagonist
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases .
|
-
- HY-P10422
-
|
ML-peptide, Multi-Leucine (ML)-peptide
|
Peptides
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-P10313
-
|
[Nle8'18,Tyr34]bPTH (3-34) amide
|
Peptides
|
Others
|
|
[Nle8,18,Tyr34]-pTH (3-34) amide (bovine) ([Nle8'18,Tyr34]bPTH (3-34) amide) is an analogue of parathyroid hormone (PTH), and is a competitive inhibitor of PTH-stimulated biological responses in vitro .
|
-
- HY-P1297
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect .
|
-
- HY-P2244
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 is a potent and competitive inhibitor of?YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM) .
|
-
- HY-P4522A
-
|
|
Endogenous Metabolite
|
Others
|
|
Bz-Ala-Arg TFA is a dipeptide. Bz-Ala-Arg TFA is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg TFA can be used to screen competitive inhibitors of these two enzymes .
|
-
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
|
-
- HY-106103A
-
|
MK 678 acetate; L 36358 acetate
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
|
-
- HY-P2244A
-
|
|
YAP
|
Cancer
|
|
YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of?YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM) .
|
-
- HY-106103
-
|
MK-678; L-363586
|
Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
|
|
Seglitide (MK-678) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide can be used for research on diabetes .
|
-
- HY-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation .
|
-
- HY-P0096
-
|
|
Tyrosinase
Sirtuin
|
Inflammation/Immunology
Endocrinology
|
|
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 μM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
|
-
- HY-P1297A
-
|
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect .
|
-
- HY-P3678
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure .
|
- HY-P5038
-
|
c(GRGDSP)
|
Integrin
|
Cancer
|
|
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
|
- HY-P1740A
-
|
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation .
|
- HY-P10552
-
|
|
CXCR
|
Inflammation/Immunology
|
|
pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis .
|
- HY-P1173
-
|
Myristoylated L 803; GSK-3β inhibitor XIII
|
GSK-3
Amyloid-β
|
Neurological Disease
|
|
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .
|
- HY-P10600
-
|
|
Peptides
|
Others
|
|
BIMAX2 is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
- HY-P10600A
-
|
|
Peptides
|
Others
|
|
BIMAX2 acetate is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 acetate can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 acetate can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is a competitive, irreversible pan-caspase inhibitor. Z-VAD inhibits all 10 caspases, except for caspase-2 which is only weakly inhibited. Z-VAD decreases radiation-induced apoptosis. Z-VAD induces both autophagy and necrosis in irradiated MDA-MB-231 and H460 mouse xenografts. Z-VAD with radiation produces a significant tumor growth delay and shows dramatic antiangiogenic effect in cancer xenograft .
|
- HY-P3143A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68?nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs .
|
- HY-P5322
-
|
|
Peptides
|
Others
|
|
Thrombospondin (TSP-1)-derived CD36 binding motif is a biological active peptide. (This peptide is derived from thrombospondin and represents a binding motif responsible for thrombospondin-CD36 interaction. It is cyclized through a disulfide bond. Thrombospondin is a matrix-bound glycoprotein involved in cancer metastasis, tumor adhesion, and angiogenesis. This peptide has been shown to competitively inhibit platelet aggregation and tumor metastasis.)
|
- HY-P10465
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-Tat is an antagonistic peptide that fuses the TRPV1 (transient receptor potential vanilla subtype 1) of the cell-penetrating peptide Tat. TRPV1-Tat blocks this phosphorylation process by competitively binding to the AKAP79 binding site of TRPV1, thereby inhibiting the sensitization of TRPV1. TRPV1-Tat can be used in the study of inflammatory pain .
|
- HY-P3143
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50?of 7.68?nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST?and SPR assays, respectively.?BMSpep-57?facilitates T cell function by in creasing IL-2 production in PBMCs .
|
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
|
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
|
- HY-P4160
-
|
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
- HY-P2055
-
|
|
Peptides
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-108847
-
|
|
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
|
-
- HY-P99639
-
|
APL-501; CBT-501; GB-226
|
PD-1/PD-L1
|
Cancer
|
|
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer .
|
-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-Y1787
-
-
- HY-N1860
-
-
- HY-121377
-
-
- HY-N10002
-
-
- HY-B0199A
-
-
- HY-N9685
-
-
- HY-W010510R
-
-
- HY-100397
-
|
|
Microorganisms
Source classification
|
Elastase
|
|
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
|
-
- HY-113054
-
-
- HY-N6054
-
-
- HY-N2383
-
|
(1R,2S,3S,4S,6R)-4-Amino-6-(hydroxymethyl)cyclohexane-1,2,3-triol
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Glucosidase
|
|
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme .
|
-
- HY-N1201R
-
-
- HY-N12736
-
-
- HY-20558R
-
-
- HY-N9949
-
-
- HY-13503R
-
-
- HY-135072R
-
-
- HY-116750
-
-
- HY-N6650
-
-
- HY-N4289
-
-
- HY-N10497
-
|
|
Alkaloids
Leguminosae
Plants
|
nAChR
|
|
Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced .
|
-
- HY-N7114
-
-
- HY-B0183R
-
-
- HY-18963
-
-
- HY-10963
-
-
- HY-N10488
-
-
- HY-W727627
-
-
- HY-N9075
-
-
- HY-W051513
-
-
- HY-113514
-
-
- HY-W685943
-
-
- HY-W009156
-
-
- HY-16007
-
-
- HY-113468A
-
-
- HY-100786
-
-
- HY-N1193
-
-
- HY-129137
-
|
Cy 3-soph
|
Rosaceae
Plants
Prunus cerasus L.
|
Others
|
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-W011184
-
-
- HY-126946
-
-
- HY-B1295
-
-
- HY-W661499
-
-
- HY-N0021R
-
-
- HY-N0575R
-
-
- HY-125833
-
-
- HY-135780
-
-
- HY-N8382
-
-
- HY-B0134R
-
-
- HY-N2463
-
-
- HY-130199
-
-
- HY-15141
-
-
- HY-N4193
-
-
- HY-N6057
-
-
- HY-N7377
-
-
- HY-W010378
-
-
- HY-N0793R
-
-
- HY-N7114AR
-
-
- HY-N2554
-
-
- HY-135780A
-
-
- HY-122936
-
-
- HY-B1729
-
|
|
Microorganisms
Source classification
|
Oxidative Phosphorylation
Bacterial
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-N7536
-
-
- HY-N7433
-
-
- HY-P1293
-
-
- HY-113038B
-
-
- HY-N10489
-
-
- HY-N6054R
-
-
- HY-N12761
-
-
- HY-107339
-
-
- HY-B0236
-
-
- HY-15237
-
-
- HY-N8122
-
-
- HY-113329
-
-
- HY-113038A
-
-
- HY-100513A
-
-
- HY-W009156R
-
-
- HY-101037
-
-
- HY-P1293A
-
|
|
Natural Products
Animals
Source classification
|
iGluR
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties .
|
-
- HY-114203
-
-
- HY-N1919
-
-
- HY-N1919A
-
-
- HY-N2689
-
-
- HY-N9933
-
-
- HY-N4037
-
-
- HY-W008364
-
-
- HY-N0063
-
-
- HY-N0192
-
-
- HY-17462
-
-
- HY-P99639
-
-
- HY-W015309
-
-
- HY-N1483
-
-
- HY-N10403
-
-
- HY-B0290
-
-
- HY-B1205
-
-
- HY-B0290A
-
-
- HY-131592
-
-
- HY-P99345
-
-
- HY-B1729R
-
|
|
Microorganisms
Source classification
|
Oxidative Phosphorylation
Bacterial
|
|
Phenoxyethanol (Standard) is the analytical standard of Phenoxyethanol. This product is intended for research and analytical applications. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al .
|
-
- HY-N4110R
-
|
|
Structural Classification
Natural Products
Celastraceae
Maytenus ilicifolia
Plants
|
Cytochrome P450
|
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-107339R
-
-
- HY-131081
-
-
- HY-16569
-
-
- HY-113038
-
-
- HY-129997
-
-
- HY-B0394
-
|
Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1205A
-
-
- HY-N10096
-
-
- HY-N12688
-
-
- HY-101037R
-
-
- HY-B0442
-
-
- HY-B0442A
-
-
- HY-B0442C
-
-
- HY-N0063R
-
|
|
Structural Classification
Punica granatum L.
Source classification
Phenols
Polyphenols
Punicaceae
Plants
|
SARS-CoV
HBV
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-W008364R
-
-
- HY-100542
-
-
- HY-W015309R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-17387
-
-
- HY-129278
-
|
|
Structural Classification
Alkaloids
Lunaria annua L.
Other Alkaloids
Source classification
Plants
Brassicaceae
|
Parasite
|
|
Lunarine is an alkaloid, which can be isolated from the seeds of kale (Lunaria annua). Lunarine lowers the blood pressure, stimulates small intestinal motility, inhibits spontaneous contractions of uterus and nervous system, and exhibits an acute toxicity with LD50 of 62.3 mg/kg in dogs and rabbits. Lunarine exhibits antiparasitic activity through a competitive inhibition of protozoan oxidoreductase trypanothione reductase (TryR) with Ki of 304 μM .
|
-
- HY-N1919R
-
-
- HY-13716
-
-
- HY-N0142
-
-
- HY-N1584
-
-
- HY-N0376
-
-
- HY-N2278
-
-
- HY-B0442B
-
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
|
Cholinesterase (ChE)
nAChR
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-122489A
-
|
|
Structural Classification
Alkaloids
Microorganisms
Source classification
Isoquinoline Alkaloids
|
Others
|
|
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioid Mu-1 receptor (Ki = 2.7 μM) .
|
-
- HY-N0192R
-
-
- HY-B0290R
-
-
- HY-B1205R
-
|
Tropine tropate (Standard); DL-Hyoscyamine (Standard)
|
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
Endogenous metabolite
|
mAChR
Endogenous Metabolite
|
|
Atropine (Standard) is the analytical standard of Atropine. This product is intended for research and analytical applications. Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine inhibits ACh-induced relaxations in human pulmonary veins. Atropine can be used for research of anti-myopia and bradycardia .
|
-
- HY-N11706
-
-
- HY-N1584A
-
-
- HY-16569R
-
|
|
Structural Classification
Natural Products
other families
Source classification
Plants
|
Microtubule/Tubulin
NOD-like Receptor (NLR)
Autophagy
Apoptosis
|
|
Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .
|
-
- HY-N0241
-
-
- HY-N12109
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
|
Others
|
|
Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
|
-
- HY-101193
-
-
- HY-B1205AR
-
|
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B0394R
-
|
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-13716R
-
|
|
Structural Classification
Alkaloids
Source classification
Quinoline Alkaloids
Papaver somniferum Linn.
Plants
Papaveraceae
|
Opioid Receptor
Apoptosis
|
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
|
-
- HY-B0442R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-N0226
-
|
|
Alkaloids
Source classification
Ranunculaceae
Coptis chinensis Franch.
Plants
Isoquinoline Alkaloids
|
Cholinesterase (ChE)
Beta-secretase
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-W011428
-
|
|
Classification of Application Fields
Disease Research Fields
Cancer
|
CDK
|
|
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
|
-
- HY-N0142R
-
-
- HY-B0442BR
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
|
Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-17504A
-
|
ZD 4522
|
Classification of Application Fields
Disease Research Fields
Cancer
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-N0235
-
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Amaryllidaceae
|
nAChR
Cholinesterase (ChE)
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-N0226A
-
-
- HY-N1584AR
-
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
MARCKS
PKA
PKC
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
- HY-N2071
-
Cedrol
1 Publications Verification
(+)-Cedrol; α-Cedrol
|
Structural Classification
Cedrus deodara (Roxburgh) G. Don
Classification of Application Fields
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
|
Cytochrome P450
Fungal
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
- HY-N5072
-
|
4',6,7-Trihydroxyisoflavone
|
Flavonoids
Classification of Application Fields
Leguminosae
Glycine max (L.) merr
Source classification
Phenols
Polyphenols
Plants
Disease Research Fields
Isoflavones
Cancer
|
CDK
PI3K
PKC
|
|
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.
Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
|
-
- HY-N1957
-
-
- HY-N0235R
-
|
|
Structural Classification
Monophenols
Leguminosae
Source classification
Phenols
Psoralea corylifolia L.
Plants
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-N2071R
-
|
|
Structural Classification
Cedrus deodara (Roxburgh) G. Don
Pinaceae
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Cytochrome P450
Fungal
|
|
Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
|
-
- HY-N1957R
-
|
|
Structural Classification
Xanthones
Guttiferae
Phenols
Polyphenols
Garcinia mangostana Linn.
Plants
|
5-HT Receptor
COX
Transthyretin (TTR)
|
|
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10450S
-
|
|
|
Dapagliflozin-d5 is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor[1].
|
-
-
- HY-15656S
-
|
|
|
Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
|
-
-
- HY-B0242S1
-
|
|
|
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
|
-
-
- HY-14664AS
-
|
|
|
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
|
-
-
- HY-14806S1
-
|
|
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
-
- HY-14806S
-
|
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
-
- HY-B0882S
-
|
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
-
- HY-17502S
-
|
|
|
Simvastatin-d11 is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[1][2].
|
-
-
- HY-17502S1
-
|
|
|
Simvastatin-d3 is the deuterium labeled Simvastatin[1]. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[2].
|
-
-
- HY-N1201S
-
|
|
|
Apigenin-d5 is a deuterated labeled Apigenin . Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
|
-
-
- HY-B0165CS
-
|
|
|
Pravastatin-d3 (sodium) is the deuterium labeled Pravastatin sodium salt. Pravastatin (CS-514) sodium salt is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM[1][2].
|
-
-
- HY-B0165S
-
|
|
|
Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
|
-
-
- HY-13966S
-
|
|
|
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
-
- HY-W015309S
-
|
|
|
Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
-
- HY-W015309S2
-
|
|
|
Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
-
- HY-W015309S1
-
|
|
|
Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
-
- HY-W015309S3
-
|
|
|
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
-
- HY-10255AS
-
|
|
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
-
- HY-12432S1
-
|
|
|
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
-
- HY-B0183S
-
|
|
|
Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). Ellagic acid is a natural antioxidant and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM .
|
-
-
- HY-16569S
-
|
|
|
Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
|
-
-
- HY-16569S1
-
|
|
|
Colchicine-d3 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
|
-
-
- HY-13966S2
-
|
|
|
2-Deoxy-D-glucose- 13C is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
|
-
-
- HY-15345AS
-
|
|
|
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
|
-
-
- HY-111095S2
-
|
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D-(-)-Lactic acid- 13C-1 is the 13C labeled D-(-)-Lactic acid. D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants .
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- HY-10255AS1
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Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
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- HY-D0145S
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7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
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- HY-Y0978S2
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Boc-Glycine-2- 13C is a 13C-labeled Linuron. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive a
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- HY-14660S
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Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
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- HY-10917S
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GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling .
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- HY-10163S1
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Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-10163S
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Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-13966S4
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2-Deoxy-D-glucose- 13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
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- HY-B0334AS
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Sulbactam-d5 (sodium) is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].
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- HY-B0113S
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Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
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- HY-10195BS
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Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
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- HY-144354S
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S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2[1].
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- HY-10163S2
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Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
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- HY-I0096S
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Indole-2-carboxylic acid- 13C is the 13C-labeled Indole-2-carboxylic acid. Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current[1][2].
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- HY-10163S3
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Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
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- HY-A0166S
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Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
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- HY-B0574S1
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Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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- HY-10512S
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AR-A014418-d3 is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].
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- HY-B0334AS1
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Sulbactam-d2 (sodium) is the deuterium labeled Sulbactam sodium[1]. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[2][3].
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- HY-B0199AS
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Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
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- HY-B0574S2
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Mefenamic acid- 13C6 is the 13C-labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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- HY-113468AS
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3-O-Methyldopa-d3 is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
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- HY-B0574S
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Mefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively[1][2].
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- HY-B0113S1
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Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-W011834S
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2'-O-Methylcytidine-d3 is deuterium labeled 2'-O-Methylcytidine (HY-W011834). 2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
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- HY-N6948S
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Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S4
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Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-50878S
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Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
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- HY-B0113S3
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Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-113468AS1
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3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
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- HY-17395S
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Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-17395AS
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Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-B1729S
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Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
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- HY-B1729S1
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Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol[1]. Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[2].
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- HY-13011S
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Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-13011S1
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Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-10873S
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N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
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- HY-101037S1
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Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-W758126
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(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ .
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- HY-10873S2
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N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
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- HY-103392S
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Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
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- HY-101037S
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Sarcosine- 15N is the 15N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
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- HY-B0236S1
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6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
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- HY-B0236S
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6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
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- HY-B0368S
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Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
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- HY-B0442S
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Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
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- HY-17504AS
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Rosuvastatin-d3 is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
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- HY-14281S
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Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
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- HY-10119S
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Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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- HY-116852S
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Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
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- HY-B0290S1
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Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
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- HY-N0192S
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Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
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- HY-12542S
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Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
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- HY-113038AS
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α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
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- HY-14664DS
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(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
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- HY-113038AS1
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α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
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- HY-50878AS
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Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
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- HY-14664CS
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(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
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- HY-W401531S
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(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
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- HY-W401531S1
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(R)-3-O-Methyldopa-d3 (hydrochloride) is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
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- HY-B0091S
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Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
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- HY-13635S
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Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
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- HY-B0442AS
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Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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- HY-A0009S
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Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
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- HY-17504BS2
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Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
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- HY-17387S1
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(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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- HY-13716S
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Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
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- HY-17623S
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Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
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- HY-17422S1
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Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
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- HY-101193S
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Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
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| Cat. No. |
Product Name |
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Classification |
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- HY-23460
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4-Ethynyl-L-phenylalanine
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Alkynes
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p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-23460A
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4-Ethynyl-L-phenylalanine hydrochloride
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Alkynes
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p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-104066
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Xiliertinib; HMPL-309
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Alkynes
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Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-123199
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SABA
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Azide
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Serotonin azidobenzamidine is an arylazido derivative of 5-hydroxytryptamine (HY-B1473A). Serotonin azidobenzamide competitively inhibits [3H]5-hydroxytryptamine uptake by rat cortical synaptosomes in the dark with a Ki of 130 nM .
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- HY-104066A
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Xiliertinib tartrate; HMPL-309 tartrate
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Alkynes
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Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-146691
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Alkynes
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hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-149880
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Alkynes
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c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-W011834
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Nucleosides and their Analogs
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2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
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- HY-13859
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L-FMAU
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Nucleosides and their Analogs
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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
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- HY-W097792
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5'-O-DMT-dU
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Nucleoside Phosphoramidites
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5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
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