Search Result
Results for "
less active
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-107777A
-
|
Others
|
Cancer
|
LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .
|
-
-
- HY-43913
-
|
Eukaryotic Initiation Factor (eIF)
|
Others
|
(R)-eIF4A3-IN-2 is a less active enantiomer of eIF4A3-IN-2. eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM .
|
-
-
- HY-14864A
-
-
-
- HY-13735C
-
|
Bacterial
|
Infection
|
l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.
|
-
-
- HY-17044A
-
IPI-145 R enantiomer; INK1197 R enantiomer
|
PI3K
|
Cancer
|
Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
|
-
-
- HY-13079
-
GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)
|
MEK
|
Cancer
|
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
|
-
-
- HY-100029B
-
|
HBV
|
Infection
|
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
|
-
-
- HY-125784A
-
|
5-HT Receptor
|
Neurological Disease
|
(R)-Viloxazine hydrochloride is a less active R-isomer of Viloxazine hydrochloride. Viloxazine hydrochloride is an effective antidepressant agent .
|
-
-
- HY-14645B
-
rel-DHMEQ
|
NF-κB
|
Cancer
|
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ.
|
-
-
- HY-114673
-
|
Neurokinin Receptor
|
Others
|
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P .
|
-
-
- HY-124909
-
-
-
- HY-U00008
-
CP 28888-27
|
IFNAR
|
Infection
|
CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
|
-
-
- HY-100423A
-
KPT-8602 (Z-isomer)
|
CRM1
|
Cancer
|
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
|
-
-
- HY-12872B
-
EGF816 (S-enantiomer)
|
EGFR
|
Others
|
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
|
-
-
- HY-120813A
-
URB913 (enantiomer)
|
Others
|
Inflammation/Immunology
|
ARN 077 enantiomer (19) is the less active enantiomer of ARN 077, with an IC50 of 3.53 μM for rat NAAA .
|
-
-
- HY-145009
-
|
STING
|
Others
|
SN-008, a less active SN-011 analog, can be used as a negative control .
|
-
-
- HY-18767A
-
-
-
- HY-100742B
-
-
-
- HY-N0756A
-
L-(-)-Bornyl acetate
|
Fungal
|
Infection
|
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .
|
-
-
- HY-16901A
-
ND-630 (S enantiomer); GS-0976 (S enantiomer); NDI-010976 (S enantiomer)
|
Acetyl-CoA Carboxylase
|
Others
|
Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase (ACC) inhibitor.
|
-
-
- HY-101682B
-
|
Others
|
Cardiovascular Disease
Others
|
(R)-SCH 42495 is the less active enantiomer of SCH 42495 . SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester proagent of SCH 42354 .
|
-
-
- HY-14855A
-
(S)-TR 700; (S)-DA 7157
|
Bacterial
Antibiotic
|
Infection
|
(S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer.
|
-
-
- HY-B2111
-
-
-
- HY-15853A
-
-
-
- HY-40354B
-
|
JAK
|
Inflammation/Immunology
|
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-40354D
-
|
JAK
|
Inflammation/Immunology
|
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-10502A
-
IND-58359 S enantiomer; (S)-(-)-R-115777
|
Farnesyl Transferase
|
Cancer
|
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
|
-
-
- HY-16715
-
-
-
- HY-16950B
-
(E)-Afimoxifene
|
Estrogen Receptor/ERR
|
Cancer
|
(E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
|
-
-
- HY-112218A
-
|
Bcl-2 Family
|
Cancer
|
(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
|
-
-
- HY-12279F
-
TGR-1202 R-enantiomer; RP5264 R-enantiomer
|
PI3K
|
Cancer
|
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
|
-
-
- HY-40354C
-
|
JAK
|
Inflammation/Immunology
|
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-12993B
-
A-60444 (R enantiomer)
|
RSV
|
Infection
|
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
|
-
-
- HY-101281B
-
|
Others
|
Neurological Disease
|
(R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC50>10 μM) .
|
-
-
- HY-112895A
-
|
Androgen Receptor
|
Cancer
|
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer .
|
-
-
- HY-B0106A
-
UCB 6474
|
Calcium Channel
|
Neurological Disease
|
Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
|
-
-
- HY-100664
-
-
-
- HY-133016A
-
|
MetAP
|
Others
|
(R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor .
|
-
-
- HY-18715
-
(S)-Ornidazole; Levornidazole
|
Bacterial
Parasite
|
Infection
|
Ornidazole Levo- is the levo-isomer of Ornidazole. Ornidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Ornidazole Levo- is the less active isomer.
|
-
-
- HY-12481A
-
|
Others
|
Cancer
|
SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.
|
-
-
- HY-W074930
-
(S)-GS 1278; (S)-PMPA; (S)-TDF
|
HIV
HBV
|
Infection
|
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .
|
-
-
- 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-15145A
-
|
Sirtuin
Autophagy
|
Metabolic Disease
|
SRT 1720 dihydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3 .
|
-
-
- HY-15145
-
|
Sirtuin
Autophagy
|
Metabolic Disease
|
SRT 1720 monohydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3 .
|
-
-
- HY-12305A
-
(R)-QVD-OPH; (R)-Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Apoptosis
|
Cancer
|
(R)-Q-VD-OPh ((R)-QVD-OPH) is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible pan-caspase inhibitor with potent antiapoptotic properties.
|
-
-
- HY-13749C
-
(S)-MK-0431 phosphate
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
|
(S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
|
-
-
- HY-100540C
-
GCA-1
|
Others
|
Infection
|
Golgicide A-1 (GCA-1) is a less active cis-diastereomer of Golgicide A (GCA). Golgicide A-1 weakly inhibits mosquito reproduction .
|
-
-
- HY-114277B
-
AMG-510 isomer
|
Others
|
Others
|
Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.
|
-
-
- HY-U00417
-
|
Ras
|
Cancer
|
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
|
-
-
- HY-122808
-
|
mGluR
|
Metabolic Disease
|
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1 .
|
-
- HY-19414A
-
-
- HY-122167
-
-
- HY-18018
-
RN486
3 Publications Verification
|
Btk
|
Inflammation/Immunology
|
RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research .
|
-
- HY-W067479
-
|
Insecticide
|
Others
|
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effective as a non-lethal chemical repellent suitable for reducing avian pest damage .
|
-
- HY-N0756AR
-
|
Fungal
|
Infection
|
(-)-Bornyl acetate (Standard) is the analytical standard of (-)-Bornyl acetate. This product is intended for research and analytical applications. (-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .
|
-
- HY-124464
-
-
- HY-15084A
-
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
|
-
- HY-101140A
-
-
- HY-19908B
-
|
Others
|
Metabolic Disease
|
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM .
|
-
- HY-134775A
-
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM .
|
-
- HY-U00193
-
|
Others
|
Metabolic Disease
|
Ro18-5362 is the less active proagent of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H ++K +)-ATPase activity and associated proton translocation.
|
-
- HY-10791
-
-
- HY-17463
-
-
- HY-100729
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively .
|
-
- HY-100729A
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively .
|
-
- HY-131328A
-
(R)-LOXO-305
|
Btk
|
Others
|
(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations .
|
-
- HY-106050
-
Wy 18251
|
Others
|
Inflammation/Immunology
Cancer
|
Tilomisole (Wy 18251) is a benzimidazothiazole experimental agent with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation .
|
-
- HY-B0106AR
-
|
Calcium Channel
|
Neurological Disease
|
Etiracetam (Standard) is the analytical standard of Etiracetam. This product is intended for research and analytical applications. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
|
-
- HY-141454
-
-
- HY-141454A
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM) .
|
-
- HY-145817B
-
(R)-RP-6306
|
Wee1
|
Cancer
|
(R)-lunresertib can be used for the research of Myt1 mediated diseases and kinds of cancer for slowing the progression of cancer . (R)-lunresertib (IC50=1360nM) is less active than (S)-lunresertib (IC50<10nM).
|
-
- HY-W394903
-
|
JAK
Drug Metabolite
|
Cancer
|
GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
|
-
- HY-101533B
-
|
Bcl-2 Family
|
Cancer
|
AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. AZD-5991 S-enantiomer is a Mcl-1 inhibitor with an IC50 of 6.3 μM in FRET assay and a Kd of 0.98 μM in surface plasmon resonance (SPR) assay.
|
-
- HY-122096
-
DCLX069
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects .
|
-
- HY-100740C
-
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM .
|
-
- HY-13728A
-
(R)-ZD 9331; (R)-BGC9331
|
Biochemical Assay Reagents
|
Cancer
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed 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-15652
-
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
|
-
- HY-108425A
-
|
Sodium Channel
|
Neurological Disease
|
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
|
-
- HY-10087
-
Navitoclax
Maximum Cited Publications
92 Publications Verification
ABT-263
|
Bcl-2 Family
|
Cancer
|
Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
|
-
- 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-12515B
-
(S)-YC-93 free base
|
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
|
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure .
|
-
- HY-112475
-
|
Tie
FLT3
|
Cancer
|
Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects .
|
-
- HY-14922
-
|
Reverse Transcriptase
HIV
|
Infection
|
Fosalvudine tidoxil is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Fosalvudine tidoxil is a prodrug derived from Alovudine (HY-B1516). Fosalvudine tidoxil is less toxic than Alovudine and can be used for the research of HIV-1 infection .
|
-
- HY-W074930R
-
|
HIV
HBV
|
Infection
|
(S)-Tenofovir (Standard) is the analytical standard of (S)-Tenofovir. This product is intended for research and analytical applications. (S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .
|
-
- HY-14877
-
-
- HY-136063
-
|
Fungal
Cytochrome P450
|
Infection
|
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM) .
|
-
- HY-147829
-
|
Carbonic Anhydrase
|
Cancer
|
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II .
|
-
- HY-D1517
-
|
Fluorescent Dye
|
Others
|
FM 2-10 is a fluorescent dye. FM 2-10 is a less hydrophobic version of FM 1-43 (HY-D1434). FM 2-10 can be used for identifying actively firing neurons and investigating the mechanisms of activity-dependent vesicle cycling .
|
-
- HY-14877A
-
SK-0403 hydrochloride
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
Metabolic Disease
|
Anagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively .
|
-
- HY-160440
-
|
Others
|
Others
|
rel-VU6021625 is the less active relative configuration of VU6021625 (HY-160440A). VU6021625 is a potent and selective mAChR M4 antagonist with IC50 values of 0.44 nM and 57 nM for human M4, rat M4, respectively .
|
-
- HY-13749CR
-
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
|
(S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
|
-
- HY-134753
-
4-Amino-N-(4-trifluoromethylphenyl)benzamide
|
COX
|
Inflammation/Immunology
|
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) is a selective COX-1 inhibitor with an IC50 of 30 µM. Teriflunomide impurity 3 is less active against COX-2 (IC50>100 µM) .
|
-
- HY-N1778A
-
(E)-O-Methylferulic acid
|
Reactive Oxygen Species
Virus Protease
|
Infection
Cancer
|
(E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway . Anti-apoptotic effects .
|
-
- HY-16723A
-
(R)-TV 45070; (R)-XEN402
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
|
-
- HY-123905A
-
|
Others
|
Cancer
|
LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM .
|
-
- HY-114577
-
Isophosphoramide mustard tromethamine; IPM tromethamine; ZIO-201 tromethamine
|
DNA Alkylator/Crosslinker
|
Cancer
|
Palifosfamide (tromethamine) is a synthetic alkylating agent with potential antineoplastic activity. As the stabilized active metabolite of ifosfamide, palifosfamide (tromethamine) irreversibly alkylates and crosslinks DNA through GC base pairs. This leads to an inhibition of DNA replication and ultimately cell death. Compared to ifosfamide, palifosfamide (tromethamine) is less toxic.
|
-
- HY-10087A1
-
ABT-263 dihydrochloride
|
Bcl-2 Family
|
Cancer
|
Navitoclax (ABT-263) dihydrochloride is an orally active Bcl-2 inhibitor that binds to various Bcl-2 family proteins, including Bcl-xL, Bcl-2, and Bcl-w, with a Ki value of less than 1 nM. Navitoclax dihydrochloride can be used in cancer research .
|
-
- HY-106407
-
Org 4428; ADL 6906
|
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Beloxepin (Org 4428) is an orally active synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. Beloxepin shows about 100-fold less affine for other monoamine carriers. Beloxepin has antidepressant and pain-relieving effects .
|
-
- HY-107429
-
PF-04965842
|
JAK
|
Inflammation/Immunology
|
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-15652A
-
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
|
-
- HY-12515C
-
(R)-YC-93 free base
|
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
|
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure .
|
-
- HY-115688A
-
|
Others
|
Cardiovascular Disease
Others
|
(S)-TXNIP-IN-1 is the less active S-enantiomer of TXNIP-IN-1 (HY-115688). TXNIP-IN-1 is a TXNIP-TRX complex inhibitor which can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease
|
-
- HY-114205
-
|
Epigenetic Reader Domain
|
Cancer
|
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-N0136B
-
(-)-Dihydroquercetin
|
Tyrosinase
|
Inflammation/Immunology
|
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-114205A
-
|
Epigenetic Reader Domain
|
Cancer
|
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-101093B
-
|
PD-1/PD-L1
|
Cancer
|
PD-1-IN-20 is the less active enantiomer of PD-1-IN-1. PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO 2015033299 A1, compound example 4 .
|
-
- HY-100013B1
-
|
Others
|
Neurological Disease
|
(1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
|
-
- HY-116830A
-
|
GSK-3
|
Cancer
|
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-111532B
-
|
ClpP
|
Infection
|
(3S,4S)-A2-32-01 (compound 24(S,S)), a less active (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protein proteases (ClpP) inhibitor .
|
-
- 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-A0295
-
-
- HY-17463R
-
|
Glucocorticoid Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Endocrinology
|
Prednisolone (Standard) is the analytical standard of Prednisolone. This product is intended for research and analytical applications. Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research .
|
-
- HY-155190
-
|
Bacterial
|
Infection
|
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM .
|
-
- HY-130696
-
(+)-Trans-(1R,2R)-U-50488
|
Opioid Receptor
|
Neurological Disease
|
(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
|
-
- HY-15997A
-
(+)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
|
-
- HY-18679
-
|
mGluR
|
Neurological Disease
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
|
-
- HY-103258
-
|
MAP3K
Apoptosis
|
Cancer
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
|
-
- 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-108235C
-
(R)-AZD6765
|
iGluR
|
Neurological Disease
|
(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects .
|
-
- HY-107429R
-
|
JAK
|
Inflammation/Immunology
|
Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-112704
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity .
|
-
- HY-122114
-
|
Potassium Channel
|
Neurological Disease
|
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects .
|
-
- HY-160111
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
PDM-042 is a potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor. PDM-042 shows potent inhibitory activities for human and rat PDE10A with IC50 values of less than 1 nM and more than 1000-fold selectivity against other phosphodiesterases. PDM-042 can be used for the research of schizophrenia .
|
-
- HY-131312
-
LY3410738; Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
|
-
- HY-50901
-
AE 3-208
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer .
|
-
- HY-12885C
-
ADU-S100 enantiomer ammonium salt; MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt
|
Others
|
Inflammation/Immunology
|
2’3’-c-di-AM(PS)2 (Rp,Rp) enantiomer ammonium salt (ADU-S100 enantiomer ammonium salt) is the less active enantiomer of 2’3’-c-di-AM(PS)2 (Rp,Rp). 2’3’-c-di-AM(PS)2 (Rp,Rp) is an activator of stimulator of interferon genes (STING) .
|
-
- HY-126047B
-
|
NF-κB
Amyloid-β
nAChR
|
Neurological Disease
Inflammation/Immunology
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
|
-
- HY-115553
-
|
Dopamine Receptor
|
Neurological Disease
|
DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor .
|
-
- HY-119530
-
BW 57-323
|
Others
|
Others
|
Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-109015
-
Chidamide; HBI-8000; CS 055
|
HDAC
|
Cancer
|
Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 .
|
-
- HY-100764
-
|
Histone Demethylase
|
Cancer
|
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity .
|
-
- HY-U00050
-
E-10-OH-NT
|
Drug Metabolite
|
Neurological Disease
|
(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline (HY-B1417). Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline (HY-B0527A) . E-10-OH-NT is about 50% as potent as nortriptyline as an inhibitor of the neuronal uptake of norepinephrine in vitro and exhibits less anticholinergic effects in man.
|
-
- HY-129388A
-
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-120982
-
|
Prostaglandin Receptor
|
Endocrinology
|
Cloprostenol is a synthetic prostaglandin F2α (PGF2α) analog and a potent FP receptor agonist. (+)-15-epi Cloprostenol is the 15(S), or 15β-hydroxy enantiomer of (+)-cloprostenol. This epimer is less active by several orders of magnitude as an FP receptor ligand when compared to 15(R)-cloprostenol. However, the specific activity of this isomer has not been well studied.
|
-
- HY-129388B
-
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-19985A
-
|
EGFR
|
Cancer
|
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
|
-
- HY-117621
-
|
CCR
|
Metabolic Disease
|
PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
|
-
- HY-157929
-
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
|
-
- HY-14201
-
Ro 19-6327
|
Monoamine Oxidase
|
Neurological Disease
|
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide ?inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and?alzheimer′s disease .
|
-
- HY-129388
-
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-14202
-
Ro 19-6327 hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
|
-
- HY-117621A
-
|
CCR
|
Metabolic Disease
|
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy .
|
-
- HY-135331
-
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
|
-
- HY-14327
-
|
Dopamine Receptor
|
Neurological Disease
|
FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic .
|
-
- HY-12119
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-109086
-
JNJ-40346527; JNJ-527
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-12119A
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-118521
-
|
PI3K
|
Inflammation/Immunology
|
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects .
|
-
- HY-141848A
-
|
mGluR
|
Neurological Disease
|
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor . BMS-984923 is a potent mGluR5 silent allosteric modulator . (S,S)-BMS-984923 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-12119B
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 (dihydrochloride) is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 (dihydrochloride) displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 (dihydrochloride) exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-109086A
-
JNJ-40346527 hydrochloride; JNJ-527 hydrochloride
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Edicotinib hydrochloride is a potent, selective, brain penetrant and orally active?colony-stimulating factor-1 receptor (CSF-1R)?inhibitor with an IC50 of 3.2 nM. Edicotinib hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-119530R
-
|
Others
|
Others
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-135976
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25?nM, 92?nM and 126?nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
|
-
- HY-120179A
-
|
AAK1
|
Neurological Disease
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
|
-
- HY-100218B
-
|
Others
|
Cancer
|
(1R,3S)-RSL3 is the less active (1R,3S)-enantiomer of RSL3 ((1S,3R)-RSL3). (1R,3S)-RSL3 and RSL3 induce cell death in HT22 wild-type cells with EC50 values of 5.2 µM and 0.004 µM, rspectively .
|
-
- HY-50751
-
ABT-869; AL-39324
|
PDGFR
VEGFR
FLT3
c-Fms
c-Kit
Autophagy
Apoptosis
|
Cancer
|
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .
|
-
- 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-111754
-
|
MAP4K
|
Cardiovascular Disease
|
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice .
|
-
- HY-111540B
-
(S)-IDO1-IN-5
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
(S)-LY-3381916 ((S)-IDO1-IN-5; Example 1B) is an active S-isomer of LY-3381916. (S)-LY-3381916 binds to IDOL with an IC50 value less than 1.5 µΜ . LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .
|
-
- HY-10181G
-
BMS-354825 (GMP)
|
Src
Bcr-Abl
Apoptosis
Autophagy
|
Cancer
|
Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy .
|
-
- HY-147041
-
GB1211
|
Galectin
|
Inflammation/Immunology
Cancer
|
Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis .
|
-
- HY-111052
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
|
-
- HY-13224A
-
|
Endogenous Metabolite
|
Cancer
|
AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
|
-
- HY-135699
-
TD52
1 Publications Verification
|
Apoptosis
Phosphatase
Akt
|
Cancer
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 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-135699A
-
|
Akt
Phosphatase
Apoptosis
|
Cancer
|
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) 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-120973
-
|
Biochemical Assay Reagents
|
Others
|
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
|
-
-
-
HY-L096
-
|
173 compounds
|
An inactive ingredient is any component of a drug product other than the active ingredient. Inactive ingredients are added during the manufacturing process of pharmaceutical products such as tablets, capsules, suppositories, and injections. In new drug development, once an inactive ingredient has appeared in an approved drug product for a particular route of administration, the inactive ingredient is not considered new and may require a less extensive review the next time it is included in a new drug product.
MCE offers a unique collection of 173 inactive ingredients, which only contain inactive ingredients of the final dosage forms of the drug. MCE Inactive Ingredient library is a powerful tool for aiding in the development of the drug and saving unnecessary time.
|
Cat. No. |
Product Name |
Type |
-
- HY-D1517
-
|
Fluorescent Dyes/Probes
|
FM 2-10 is a fluorescent dye. FM 2-10 is a less hydrophobic version of FM 1-43 (HY-D1434). FM 2-10 can be used for identifying actively firing neurons and investigating the mechanisms of activity-dependent vesicle cycling .
|
Cat. No. |
Product Name |
Type |
-
- HY-120973
-
|
Biochemical Assay Reagents
|
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2678
-
|
Peptides
|
Metabolic Disease
|
CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
|
Classification |
-
- HY-135699
-
TD52
1 Publications Verification
|
|
Alkynes
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 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-135699A
-
|
|
Alkynes
|
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) 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-13728A
-
(R)-ZD 9331; (R)-BGC9331
|
|
Alkynes
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: