Search Result
Results for "
concentration-dependent
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B2179
-
-
-
- HY-B2133
-
-
-
- HY-U00027
-
-
-
- HY-100407
-
|
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
-
- HY-N7483
-
|
|
Others
|
Metabolic Disease
|
|
1-Dehydroxybaccatin IV is a taxane diterpene. 1-Dehydroxybaccatin IV shows concentration-dependent NO inhibition, with an IC50 of 32.2 μM .
|
-
-
- HY-N2929
-
|
|
Glucosidase
|
Cardiovascular Disease
|
|
β-Hydroxypropiovanillone, a natural compound, shows significant concentration-dependent inhibitory effects on α-glucosidase with an IC50 of 257.8 μg/mL .
|
-
-
- HY-131871
-
-
-
- HY-N5035
-
|
Plicatol B
|
Others
|
Cardiovascular Disease
|
|
Moscatin inhibits AA-induced platelet aggregation in a concentration-dependent manner with IC50 values 37.2 μM .
|
-
-
- HY-19583
-
-
-
- HY-116850
-
|
EG626; Phthalazinol; SC-32840
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Oxagrelate is a specific inhibitor of cyclic adenosine monophosphate phosphodiesterase and exhibits concentration-dependent inhibition of collagen- and ADP-induced platelet aggregation in vitro .
|
-
-
- HY-121026
-
-
-
- HY-123175
-
|
|
Others
|
Others
|
|
Chinfloxacin is a compound with antibacterial activity. It is active against a variety of clinical isolates in vitro. Its antibacterial activity is similar to that of moxifloxacin, and it has a bactericidal effect in a concentration-dependent manner.
|
-
-
- HY-109066
-
|
IW-1701
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay .
|
-
-
- HY-N12737
-
|
|
Others
|
Inflammation/Immunology
|
|
15-epi-Danshenol A is a diterpenoid with an immune-modulating activity. 15-epi-Danshenol A shows inhibitory effect on B lymphoblasts cells in a concentration-dependent manner .
|
-
-
- HY-B2133R
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
Cloperastine (hydrochloride) (Standard) is the analytical standard of Cloperastine (hydrochloride). This product is intended for research and analytical applications. Cloperastine hydrochloride inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM .
|
-
-
- HY-N10117
-
|
|
RANKL/RANK
|
Others
|
|
2,3-Bis(3-indolylmethyl)indole significantly suppresses RANKL-induced osteoclast formation, actin ring formation, and bone resorption in a concentration-dependent manner.
|
-
-
- HY-10562
-
-
-
- HY-B0267AS
-
-
-
- HY-14304
-
|
MJ 9184
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol (MJ 9184) is a potent and selective β2-adrenoceptor agonist . Zinterol increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM .
|
-
-
- HY-N1210
-
|
Spiramine C acetate (ester)
|
Bacterial
|
Cancer
|
|
Spiramine A (Spiramine C acetate (ester)) is a diterpene alkaloid with antitumor and antimicrobial activity. Spiramine A inhibits PAF-induced rabbit platelet aggregation in a concentration-dependent manner, with an IC50 vallue of 6.7 μM .
|
-
-
- HY-N4053
-
-
-
- HY-14276
-
|
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist . Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM . Gallopamil is a potent antiarrhythmic and vasodilator agent .
|
-
-
- HY-14276A
-
|
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist . Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM . Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent .
|
-
-
- HY-119124
-
|
D21-2393
|
Drug Metabolite
|
Metabolic Disease
|
|
Edoxaban M4, an active metabolite of Edoxaban, shows reproducible, but concentration-dependent matrix effects. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor .
|
-
-
- HY-U00201
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
KRN4884 is a K + channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
|
-
-
- HY-P1236
-
|
Atrial natriuretic factor (1-28) (rat, mouse)
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
-
- HY-10562A
-
-
-
- HY-P1236A
-
|
Atrial natriuretic factor (1-28) (rat, mouse) TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
-
- HY-101436
-
|
CK-1752
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent .
|
-
-
- HY-101436A
-
|
CK-1752 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent .
|
-
-
- HY-121710
-
|
7-Monohydroxyethylrutoside
|
Others
|
Cardiovascular Disease
|
|
MonoHER (7-Monohydroxyethylrutoside) is a Carbonyl reductase 1 (CBR1) inhibitor and can be used as a cardioprotective agent. MonoHER inhibits the activity of CBR1 V88 and CBR1 I88 in a concentration-dependent manner .
|
-
-
- HY-P2206
-
|
|
Bacterial
|
Infection
|
|
Zelkovamycin is a cyclic peptide antibiotic originally isolated from Streptomyces. It inhibits growth of X. oryzae, P. oryzae, S. aureus, and A. laidlawii in a concentration-dependent manner when used at concentrations ranging from 0.01 to 300 μg/mL.
|
-
-
- HY-18719
-
|
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
|
Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
|
-
-
- HY-N9506
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM .
|
-
-
- HY-N3464
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity .
|
-
-
- HY-110180
-
|
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
|
-
-
- HY-156398
-
|
|
NO Synthase
β-catenin
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 60(compound 21) inhibitsnitric oxide production, with anIC50value of 12.95 μM.Anti-inflammatory agent 60reducesiNOS,phosphorylated p65, andβ-cateninexpression in a concentration-dependent manner .
|
-
-
- HY-14304A
-
|
MJ 9184 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist . Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM . Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits .
|
-
-
- HY-N8475
-
|
|
PKC
|
Cancer
|
|
6-Deoxyisojacareubin is a PKC inhibitor that inhibits the proliferation of QGY-7703 cells in a concentration-dependent manner. 6-Deoxyisojacareubin is also a natural product that can be obtained from Garcinia nervosa. 6-Deoxyisojacareubin can be used in cancer research .
|
-
-
- HY-10562R
-
|
|
5-HT Receptor
Potassium Channel
Autophagy
|
Neurological Disease
|
|
Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
|
-
-
- HY-N6679
-
|
|
Antibiotic
|
Cancer
|
|
(R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines
with a mean IC50 value of 1.25 µM .
|
-
-
- HY-101303
-
|
|
Melatonin Receptor
|
Others
|
|
5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP .
|
-
-
- HY-113269
-
|
|
Others
|
Others
|
|
alpha-CEHC is a water-soluble metabolite of alpha-tocopherol (α-TOH) with potential antioxidant activity. alpha-CEHC slightly inhibits macrophage-induced low-density lipoprotein (LDL) oxidation, and its inhibitory potency is concentration-dependent .
|
-
-
- HY-B0267
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
Cancer
|
|
Oxybutynin is an anticholinergic agent, which inhibits vascular Kv channels in a concentration-dependent manner, with an IC50 of 11.51 μM . Oxybutynin 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-10174
-
|
|
MEK
Apoptosis
|
Neurological Disease
Cancer
|
|
PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior .
|
-
-
- HY-D1876
-
|
|
Fluorescent Dye
|
Cancer
|
|
ZY-2 is a specific fluorescent probe for pyruvate kinase M2 (PKM2). ZY-2 can image in PKM2-positive cells in a time- and concentration-dependent manner. ZY-2 can be used for the detection of cancer cells .
|
-
-
- HY-146711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
|
-
-
- HY-146735
-
|
|
MNK
Apoptosis
|
Cancer
|
|
MNK1/2-IN-6 is a potent and selective MNK1/2 inhibitor with IC50s of 2.3 nM and 3.4 nM for MNK1 and MNK2, respectively. MNK1/2-IN-6 induces apoptosis in a concentration-dependent manner .
|
-
-
- HY-106323
-
|
KW-5139
|
Motilin Receptor
|
Metabolic Disease
|
|
[Leu13]-Motilin (KW-5139) is a motilin analogue. [Leu13]-Motilin stimulates gastrointestinal motility in the rabbit. [Leu13]-Motilin causes concentration-dependent contractions of the gastric antrum, duodenum, jejunum, ileum and the descending colon in vitro .
|
-
![[Leu13]-Motilin](//file.medchemexpress.eu/product_pic/hy-106323.gif)
-
- HY-150092
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
8(S),9(R)-EET is an eicosanoid product of Arachidonic acid (AA; HY-109590) by cytochromes P450. 8(S),9(R)-EET dilates canine epicardial arterioles in a concentration-dependent manner with an EC50 value of 121 nM .
|
-
- HY-13289A
-
|
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB) .
|
-
- HY-13103
-
|
|
Potassium Channel
|
Others
|
|
NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials .
|
-
- HY-114920
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Piprofurol is a calcium channel inhibitor. Piprofurol inhibits the calcium-induced contractions in isolated potassium depolarized preparations of rat aorta in a concentration-dependent manner and relaxes the K +-induced contraction of the dog coronary artery and the rabbit basilar artery. Piprofurol exerts a negative inotropic effect on guinea-pig papillary muscle, with the EC50 of 5 μM .
|
-
- HY-19517
-
|
|
Others
|
Cardiovascular Disease
|
|
R1663 is a factor Xa inhibitor with anticoagulant activity. R1663 does not affect bleeding time. The pharmacodynamic effects (such as inhibition of thrombin generation) and plasma concentrations of R1663 are dose-dependent. R1663 prolongs clotting time in a concentration-dependent manner and inhibits the peak height of thrombin generation and endogenous thrombin potential .
|
-
- HY-153542
-
|
|
Others
|
Others
|
|
AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition .
|
-
- HY-13289
-
|
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) .
|
-
- HY-106668
-
|
Sch 21420
|
Antibiotic
Bacterial
|
Infection
|
|
Isepamicin (Sch 21420) is an aminoglycoside antibacterial. Isepamicin has better activity against strains producing type I 6'-acetyltransferase. Isepamicin’s antibacterial spectrum includes Enterobacteriaceae and staphylococci. Anaerobes, Neisseriaceae and streptococci are resistant. Isepamicin exhibits a strong concentration-dependent bactericidal effect, a long post-antibiotic effect (several hours) and induces adaptive resistance .
|
-
- 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-160259
-
|
|
PROTACs
VEGFR
|
Cardiovascular Disease
|
|
VEGFR-2-IN-39 (PROTAC-5) is a PROTAC targeting VEGFR-2 (IC50: 208.6 nM). VEGFR-2-IN-39 has low toxicity.VEGFR-2-IN-39 inhibits the proliferation of EA.hy926, one of HUVECs, in a concentration-dependent manner, with an IC50 of 38.65 µM .
|
-
- HY-B0267R
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin (Standard) is the analytical standard of Oxybutynin. This product is intended for research and analytical applications. Oxybutynin is an anticholinergic agent, which inhibits vascular Kv channels in a concentration-dependent manner, with an IC50 of 11.51 μM . Oxybutynin 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-B0189
-
|
TAK-370; AS-4370
|
5-HT Receptor
Cytochrome P450
Potassium Channel
|
Neurological Disease
Cancer
|
|
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
|
-
- HY-B0189A
-
|
TAK-370 citrate; AS-4370 citrate
|
5-HT Receptor
Potassium Channel
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .
|
-
- HY-N0245
-
|
|
Others
|
Cancer
|
|
Theaflavin-3-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3-gallate reacts directly with reduced glutathione (GSH) in a time- and concentration-dependent manner .
|
-
- HY-103212
-
|
B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively . Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM) .
|
-
- HY-105064
-
|
CP-597396
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) is a potent and selective NHE-1 inhibitor with cardioprotective activity. Zoniporide inhibits 22Na + uptake by human NHE-1-expressing fibroblasts in a concentration-dependent manner (IC50=14 nM). Zoniporide inhibits platelet swelling in vitro with an IC50 of 0.059 μM. Zoniporide can be used in the study of cardiovascular disease .
|
-
- HY-106004
-
|
BIA 5-1058
|
Dopamine β-hydroxylase
P-glycoprotein
BCRP
|
Cardiovascular Disease
Cancer
|
|
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively . Zamicastat reduces high blood pressure .
|
-
- HY-144321
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
|
-
- HY-N1735
-
|
|
Bacterial
Others
|
Inflammation/Immunology
|
|
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively .
|
-
- HY-168167
-
|
|
Others
|
Neurological Disease
|
|
BuChE-IN-14 is a novel compound that selectively inhibits acetylcholinesterase (AChE) activity. BuChE-IN-14 showed a concentration-dependent inhibitory effect on AChE in rat brain in vitro experiments. BuChE-IN-14 can increase the extracellular acetylcholine (ACh) concentration in the rat hippocampus and striatum at a certain dose. BuChE-IN-14 may help improve memory impairment caused by cholinergic dysfunction .
|
-
- HY-143447
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-8 concentration-dependently causes cell cycle arrest at the G2/M phase in HCT116 tumor cells, and displays a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM. Tubulin polymerization-IN-8 has the potential for the research of cancer diseases [ 1].
|
-
- HY-103212A
-
|
B-HT 933 hydrochloride; Oxazoloazepin hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-B0189B
-
|
TAK-370 citrate dihydrate; AS-4370 citrate dihydrate
|
5-HT Receptor
Potassium Channel
Cytochrome P450
|
Metabolic Disease
Cancer
|
|
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM . Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo .
|
-
- HY-152159
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
|
-
- HY-156908
-
|
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
3-OH-Kynurenamine is a lateral metabolite in Tryptophan (HY-N0623) metabolism. 3-OH-Kynurenamine induces a concentration-dependent AhR activation, around 6.5 times higher than L-kynurenine (HY-104026). 3-OH-Kynurenamine confers immunosuppressive properties on dendritic cells (DCs). 3-OH-Kynurenamine can be used for psoriasis research .
|
-
- HY-13289B
-
|
(R)-SYN117 hydrochloride; (R)-RS-25560-197 hydrochloride; RS-25560-198 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
(R)-Nepicastat hydrochloride is the isomer of Nepicastat (HY-13289). Nepicastat (SYN117) is a selective，potent，and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) .
|
-
- HY-111150
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasma proteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes .
|
-
- HY-113308
-
|
|
Others
|
Others
|
|
Taurolithocholic acid is a bile acid that has the activity of increasing cell viability, inducing the S phase of the cell cycle, and promoting DNA synthesis in a concentration-dependent manner in the intrahepatic cholangiocarcinoma cell line RMCCA-1. It can also increase the phosphorylation of EGFR and ERK 1/2 and the expression of cyclin D1 in RMCCA-1 cells, and its induced RMCCA-1 cell growth can be inhibited by specific antagonists and inhibitors.
|
-
- HY-122215
-
|
N-696
|
Others
|
Endocrinology
|
|
Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
|
-
- HY-104064
-
1A-116
5 Publications Verification
|
Ras
Apoptosis
|
Cancer
|
|
1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo .
|
-
- HY-120323
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively .
|
-
- HY-126052
-
|
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-156453
-
|
|
PAK
Apoptosis
|
Cancer
|
|
PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
|
-
- HY-118317
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Zacopride is a selective agonist with the activity of enhancing the inward rectifier potassium current (IK1) in rabbit hearts. Zacopride also exhibits significant antiarrhythmic effects, inhibiting ventricular arrhythmias by increasing IK1 without affecting atrial arrhythmias. Zacopride can hyperpolarize the resting membrane potential and shorten the action potential duration (APD) in a concentration-dependent manner. Zacopride significantly reduced the incidence of compound-induced early afterdepolarizations (EADs) at 1 μmol/L .
|
-
- HY-119092
-
|
|
Others
|
Cardiovascular Disease
|
|
Bisaramil is an orally active antiarrhythmic agent. Bisaramil exerts concentration dependent inhibitory effect on PMA-stimulated free radical generation and prolonged the time lag concentration dependently .
|
-
- HY-103511
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
|
-
- HY-W127408
-
|
|
Biochemical Assay Reagents
Endogenous Metabolite
|
Others
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
-
- HY-133217
-
|
|
Bacterial
|
Infection
|
|
Benastatin C is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities. It inhibits glutathione S-transferase (GST; IC50=24 μg/mL for the rat liver enzyme).2 Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50=10 μg/mL). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.
|
-
- HY-161836
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
α2AR agonist 1 (compound S6a), a new morpholine-containing pyrimidinone, acts as an agonist of α2-adrenoceptor. α2AR agonist 1 induces a concentration-dependent relaxation on aortic ring pre-contracted with Phenylephrine (HY-B0769; pEC50=6.81). α2AR agonist 1 increases NOx and NO levels in HUVECs .
|
-
- HY-131701
-
|
C18 Lactosyl(β) Ceramide; Lactosyl Sphingosine; Lyso-Lactosylceramide (synthetic)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lactosyl-C18-sphingosine (C18 Lactosyl(β) Ceramide; Lactosyl Sphingosine) is a bioactive sphingolipid that is a form of lactosylceramide but lacks the fatty acyl group. Lysolactosylceramide (1-50 μM) reduces the viability of human neutrophils in a concentration-dependent manner. Unlike lactosylceramide, Lactosyl-C18-sphingosine has no effect on protein synthesis and cell proliferation in cardiomyocytes. Lactosyl-C18-sphingosine is a lysoganglioside GM3.
|
-
- HY-W014421
-
|
|
TRP Channel
|
Neurological Disease
|
|
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
|
-
- HY-151486
-
|
|
GLUT
|
Cancer
|
|
GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC50 values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer .
|
-
- HY-P1997
-
|
Desferrichrome; DFC; N-Desferriferrichrome
|
Biochemical Assay Reagents
|
Others
|
|
Ferrichrome is a hydroxamate siderophore produced by various fungi, including U. sphaerogena, that facilitates iron chelation and uptake by these organisms. It can be used as a heterosiderophore by bacteria, including Pseudomonas aeruginosa and Vibrio parahaemolyticus. Ferrichrome (0.8 μM) inhibits concanavalin A-induced proliferation of mouse spleen monocytes and reduces the number of concanavalin A-stimulated CD4+ T cells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
|
-
- HY-162347
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
|
-
- HY-164144
-
|
|
Others
|
Cancer
|
|
EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
|
-
- HY-163481
-
|
|
Bacterial
|
Infection
|
|
Antibiofilm agent-6 (Compound 26c) is a quorum sensing inhibitor with strong antibiofilm effects that can inhibit the fluorescence intensity of PAO1-lasB-gfp and PAO1-pqsA-gfp in a concentration-dependent manner. Antibiofilm agent-6 can inhibit the production of pyocyanin and rhamnolipid. Antibiofilm agent-6 aids helps ciprofloxacin (HY-B0356) effectively eliminate the living bacteria in a mouse model infected with P. aeruginosa PAO1 .
|
-
- HY-N0244R
-
|
|
Others
|
Cancer
|
|
Theaflavin-3'-gallate (Standard) is the analytical standard of Theaflavin-3'-gallate. This product is intended for research and analytical applications. Theaflavin-3'-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3'-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3'-gallate reacts directly with reduced glutathione (GSH) in a time-and concentration-dependent manner .
|
-
- HY-117694
-
|
|
CGRP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine .
|
-
- HY-N13294
-
|
TMJ-105
|
Apoptosis
JAK
STAT
p38 MAPK
JNK
ERK
|
Cancer
|
|
Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy .
|
-
- HY-105572
-
|
MC-838 calcium
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Moveltipril calcium (MC-838 calcium) is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moveltipril calcium binds via a stable thioester bond and exhibits relative resistance to enzymatic hydrolysis in rat liver homogenate. Moveltipril calcium effectively inhibits ACE extracted from rabbit lung in a concentration-dependent manner. Moveltipril calcium is able to highly specifically inhibit the contractile response to angiotensin-I (AI) in free rat aortic rings and guinea pig ileum preparations, while enhancing the contractile response to calcitonin .
|
-
- HY-147740
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
WEHI-150 is a replica of mitoxantrone, is a portent DNA interstrand crosslinkConcentration-dependent transcription blockages. WEHI-150 can mediate covalent adducts that are independent of interactions with the N-2 of guanine and is capable of adduct formation at novel DNA sequences .
|
-
- HY-113484
-
|
LTB5
|
Others
|
Cancer
|
|
Leukotriene B5 (LTB5) is a leukotriene with diverse biological activities. It is a metabolite of eicosapentaenoic acid formed through the 5-lipoxygenase (5-LO) pathway. LTB5 increases contraction of bullfrog lung strips ex vivo in a concentration-dependent manner. In vivo, LTB5 (100 nM) reduces tumor volume in mice injected with Tm1 murine melanoma cells. LTB5 also elicits chemokinesis and lysosomal enzyme release from polymorphonuclear leukocytes (PMNLs) 20- to 30-fold less, and induces platelet aggregation 8-fold less, potently than LTB4.
|
-
- HY-118987
-
-
- HY-111844
-
|
|
PROTACs
SNIPERs
RAR/RXR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
|
-
- HY-116153
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2?/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
|
-
- HY-162888
-
|
|
PDGFR
ERK
|
Cardiovascular Disease
|
|
WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
|
-
- HY-121779
-
|
2,4'-DDE; 2,4-Dichlorodiphenyldichloroethylene; 2,4'-DDE; o,p'-Dichlorodiphenyldichloroethylene
|
Others
|
Endocrinology
|
|
o,p'-DDE (2,4-Dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT. It accumulates in smallmouth buffalo, channel catfish, and largemouth bass, and in sediments from DDT manufacturing plants around the Huntsville Spring Branch-Indian Creek tributary system, where it is considered a persistent organic pollutant (POP). o,p'-DDE inhibits estrogen binding to the rainbow trout estrogen receptor (rtER) with an IC50 value of 3.2 μM. It induces concentration-dependent estradiol secretion in co-cultures of granulosa and theca cells isolated from porcine follicles. In ovo exposure to o,p'-DDE increases follicular degeneration and reduces testis size in Japanese medaka (O. latipes).
|
-
- HY-112356
-
|
|
Apoptosis
Reactive Oxygen Species
Polo-like Kinase (PLK)
|
Inflammation/Immunology
Cancer
|
|
Scytonemin is a hydrophobic alkaloid pigment that can be isolated from the outer sheath of cyanobacteria. Scytonemin has protective function against short-wave solar ultraviolet (UV) radiation, which can reduce the generation of reactive oxygen species (ROS) and the formation of DNA damage. Scytonemin also has anti-inflammatory and anti-proliferative activities, produces concentration-dependent inhibition (IC50=2.0 μM) of polo-like kinase 1 (PLK1)-mediated cdc25C phosphorylation, and plays an important role in regulating the G2/M transition in the cell cycle. It can be used in the research of cancer, acute inflammation and sunscreen cosmetics .
|
-
- HY-136677
-
|
|
Others
|
Cardiovascular Disease
|
|
LND 796 is an aminosteroidal derivative with positive inotropic effects similar to those of digitalis. It exhibits electrophysiological, toxic, and inotropic effects in normal and partially potassium-depolarized ventricular muscles. LND 796 requires higher concentrations than digoxin to induce the same toxic symptoms. It exhibits a concentration-dependent positive inotropic effect on guinea pig papillary muscles in normal potassium solution. In partially potassium-depolarized papillary muscles, LND 796 enhances both components of contraction and increases the amplitude of slow action potentials. The mechanism of positive inotropic action of LND 796 involves enhanced calcium entry in calcium channels and inhibition of sodium-potassium ATPase. Due to its expanded positive inotropic range, LND 796 may have potential application in the treatment of congestive heart failure.
|
-
- HY-100057
-
|
6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone. It is formed from buspirone via the cytochrome P450 (CYP) isozyme CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). It also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
|
-
- HY-114796
-
|
|
Others
|
Inflammation/Immunology
|
|
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
|
-
- HY-127022A
-
|
|
Others
|
Neurological Disease
|
|
Anisodine hydrobromide is a neuroprotective compound that interacts with muscarinic receptors (M1-M5) in cerebral ischemic diseases. Anisodine hydrobromide effectively reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine hydrobromide demonstrates concentration-dependent inhibition of calcium ion influx and reactive oxygen species (ROS) levels, elucidating its neuroprotective mechanisms. Anisodine hydrobromide leads to decreased aspartate levels in HM cells during hypoxia, highlighting its effects on neurotransmitter modulation. Anisodine hydrobromide holds promising clinical prospects as a potential therapeutic agent for ischemic brain diseases, warranting further investigation into its mechanisms of action.
|
-
- HY-137325A
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
|
-
- HY-159606
-
|
|
MDM-2/p53
|
Cancer
|
|
MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53 Y220C stabilizer and targeting p53 Y220C. MS182 is composed of p53 Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53 Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53 Y220C (ACE50: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI50 values of 2.16 μM and 1.83 μM for BxPC3 (p53 Y220C/-) and NUGC (p53 Y220C/+), respectively .
|
-
- HY-12708
-
Chlorpromazine
Maximum Cited Publications
57 Publications Verification
|
Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
|
-
- HY-B0407A
-
|
|
Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-146666
-
|
|
Apoptosis
STAT
|
Cancer
|
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-W440988
-
|
|
Liposome
|
Others
|
|
DOPE-mPEG, MW 2000 is a phospholipid polydisperse PEG (or DOPE liposome), can be used for preparation of targeted delivery of liposomal drug and giant unilamellar vesicles (GUVs). DOPE-mPEG, MW 2000 significantly reduces the pH-sensitivity of the liposome in a concentration dependent manner .
|
-
- HY-119615
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist .
|
-
- HY-W013854
-
|
3β-Hydroxy-5α-androstane
|
Endogenous Metabolite
|
Others
|
|
5α-Androstan-3β-ol (Androstan), a saturated sterol, is a CAR (constitutive androstane receptor) inverse agonist ligand. 5α-Androstan-3β-ol (Androstan) increases the AmB-channel conductance in a concentration dependent manner .
|
-
- HY-118736
-
|
|
Others
|
Cardiovascular Disease
|
|
Ganodermic acid S is an oxygenated triterpenoid, that can be isolated from the Chinese medicinal fungus Ganoderma lucidum (Fr.) Karst (Polyporaceae). Ganodermic acid S exerts a concentration dependent inhibition on the response of human gel-filtered platelets (GFP) to U-46619 (HY-108566), a thromboxane (TX) A2 mimetic .
|
-
- HY-143492
-
|
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-1 (compound 14) is a potent influenza A virus inhibitor with an EC50 of 2.46 µM and CC50 of >200 µM. Influenza virus-IN-1 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 312.36 nM. Influenza virus-IN-1 shows shows anti-influenza A virus activities .
|
-
- HY-143493
-
|
|
Influenza Virus
|
Inflammation/Immunology
|
|
Influenza virus-IN-2 (compound 19) is a potent influenza virus inhibitor with an EC50 of 2.58 µM and CC50 of 150.85 µM. Influenza virus-IN-2 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 489.39 nM. Influenza virus-IN-2 shows shows anti-influenza A virus activities .
|
-
- HY-138074
-
|
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
|
Milbemycin A4 oxime is a derivative of milbemycin A4 (Item No. 17155) and a component of Milbemycin Oxime (HY-B0778), compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/mL.1 Milbemycin A4 oxime (2.5 μg/mL) blocks efflux of Fluconazole (HY-B0101) from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate Rhodamine 123 (HY-D0816), in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-B1876
-
|
|
Acetolactate Synthase (ALS)
Photosystem II
Fungal
|
Others
|
|
Nicosulfuron is efficient, harmless, antifungal and selective herbicide belonging to the sulfonylurea family. Nicosulfuron is also a photosynthetic system inhibitor and inhibits acetolactate synthase (ALS) enzyme activity. Nicosulfuron degradation by Plectosphaerella cucumerina AR1 is glucose concentration dependent in planktonic lifestyle. Nicosulfuron enhances the glycolysis pathway and tricarboxylic acid cycle to improve the adaptability of sweet maize. Nicosulfuron reduces the synthesis of branched-chain amino acids (BCAAs), which is proming for maize cultivation .
|
-
- HY-115976
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE2 in concentration dependent manner (IC50=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D1876
-
|
|
Fluorescent Dyes/Probes
|
|
ZY-2 is a specific fluorescent probe for pyruvate kinase M2 (PKM2). ZY-2 can image in PKM2-positive cells in a time- and concentration-dependent manner. ZY-2 can be used for the detection of cancer cells .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W440988
-
|
|
Drug Delivery
|
|
DOPE-mPEG, MW 2000 is a phospholipid polydisperse PEG (or DOPE liposome), can be used for preparation of targeted delivery of liposomal drug and giant unilamellar vesicles (GUVs). DOPE-mPEG, MW 2000 significantly reduces the pH-sensitivity of the liposome in a concentration dependent manner .
|
-
- HY-W127408
-
|
|
Drug Delivery
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1236
-
|
Atrial natriuretic factor (1-28) (rat, mouse)
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- 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-P5067
-
|
|
Peptides
|
Others
|
|
EAK16-II is an amphipathic peptide that inhibits the self-sorting of EAKIIH6 in a concentration-dependent manner .
|
-
- HY-P1236A
-
|
Atrial natriuretic factor (1-28) (rat, mouse) TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- HY-P2206
-
|
|
Bacterial
|
Infection
|
|
Zelkovamycin is a cyclic peptide antibiotic originally isolated from Streptomyces. It inhibits growth of X. oryzae, P. oryzae, S. aureus, and A. laidlawii in a concentration-dependent manner when used at concentrations ranging from 0.01 to 300 μg/mL.
|
-
- HY-P3562
-
|
|
Peptides
|
Others
|
|
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM .
|
-
- HY-106323
-
|
KW-5139
|
Motilin Receptor
|
Metabolic Disease
|
|
[Leu13]-Motilin (KW-5139) is a motilin analogue. [Leu13]-Motilin stimulates gastrointestinal motility in the rabbit. [Leu13]-Motilin causes concentration-dependent contractions of the gastric antrum, duodenum, jejunum, ileum and the descending colon in vitro .
|
-
- HY-P1997
-
|
Desferrichrome; DFC; N-Desferriferrichrome
|
Biochemical Assay Reagents
|
Others
|
|
Ferrichrome is a hydroxamate siderophore produced by various fungi, including U. sphaerogena, that facilitates iron chelation and uptake by these organisms. It can be used as a heterosiderophore by bacteria, including Pseudomonas aeruginosa and Vibrio parahaemolyticus. Ferrichrome (0.8 μM) inhibits concanavalin A-induced proliferation of mouse spleen monocytes and reduces the number of concanavalin A-stimulated CD4+ T cells expressing IL-2 receptor. It also inhibits the heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.
|
-
- HY-P5493
-
|
|
Peptides
|
Others
|
|
D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin is a biological active peptide. (inhibited bradykinin-induced contractions concentration dependently; bradykinin B2 receptor antagonist)
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0267AS
-
|
|
|
Oxybutynin-d11 (chloride) is the deuterium labeled Oxybutynin chloride. Oxybutynin chloride is an anticholinergic agent, which inhibits vascular Kv channels in a concentration-dependent manner, with an IC50 of 11.51 μM[1].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-118197
-
|
|
|
Azide
|
|
L-669083 is a leukotriene biosynthesis inhibitor whose structure is based on a mixture of indole and quinoline. In this study, a potent radioiodinated photoaffinity analog of L-689,037, [125I] L-691,678, was developed and characterized for immunoprecipitation studies showing that the quindole series of leukotriene biosynthesis inhibitors directly interact with FLAP. In addition, the results showed that MK-886, L-674,573, and L-689,037 competed with [125I] L-691,678 and [125I] L-669083 for binding to FLAP in a concentration-dependent manner, indicating that these three leukotriene biosynthesis inhibitors share a binding site on FLAP, further demonstrating that FLAP is a suitable target for structurally diverse leukotriene biosynthesis inhibitors.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-W440988
-
|
|
|
Pegylated Lipids
|
|
DOPE-mPEG, MW 2000 is a phospholipid polydisperse PEG (or DOPE liposome), can be used for preparation of targeted delivery of liposomal drug and giant unilamellar vesicles (GUVs). DOPE-mPEG, MW 2000 significantly reduces the pH-sensitivity of the liposome in a concentration dependent manner .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
![[Leu13]-Motilin](http://file.medchemexpress.eu/product_pic/hy-106323.gif)
