Search Result
Results for "
Isoform selectivity
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
12
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12866
-
|
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
-
- HY-13001
-
Quizartinib
Maximum Cited Publications
45 Publications Verification
AC220
|
FLT3
Apoptosis
PDGFR
c-Kit
|
Cancer
|
|
Quizartinib (AC220) is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
|
-
-
- HY-15224
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
|
-
-
- HY-17464
-
-
-
- HY-119254
-
-
-
- HY-13223
-
|
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
-
- HY-12481
-
|
|
PI3K
Autophagy
|
Cancer
|
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
|
-
-
- HY-103683
-
|
|
AMPK
|
Metabolic Disease
|
|
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
|
-
-
- HY-126585
-
SAICAR
4 Publications Verification
|
Endogenous Metabolite
|
Cancer
|
|
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
|
-
-
- HY-101972
-
-
-
- HY-15245
-
|
|
PI3K
|
Cancer
|
|
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
-
- HY-13802
-
|
GK 01140
|
IKK
|
Cancer
|
|
SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
|
-
-
- HY-109068
-
|
INCB050465; IBI-376
|
PI3K
|
Cancer
|
|
Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies .
|
-
-
- HY-16482
-
-
-
- HY-117661
-
|
|
SRPK
VEGFR
|
Cardiovascular Disease
Cancer
|
|
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease .
|
-
-
- HY-12866A
-
|
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
-
- HY-104036
-
IDH-305
4 Publications Verification
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)) .
|
-
-
- HY-126073
-
|
|
Aquaporin
|
Inflammation/Immunology
Cancer
|
|
DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 inhibits mouse and human AQP3 with an IC50 of ～0.1-0.4 μM. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9 .
|
-
-
- HY-16596
-
|
|
PI3K
|
Cancer
|
|
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
|
-
-
- HY-108318
-
-
-
- HY-108642
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
-
- HY-11010
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
-
- HY-111791
-
|
|
HDAC
|
Cancer
|
|
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
|
-
-
- HY-13531
-
|
|
PI3K
|
Cancer
|
|
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
|
-
-
- HY-107385
-
|
ONO-9302; SKF105657
|
5 alpha Reductase
|
Cancer
|
|
Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
|
-
-
- HY-14217
-
|
AC220 dihydrochloride
|
FLT3
Apoptosis
PDGFR
c-Kit
|
Cancer
|
|
Quizartinib (AC220; AC708) dihydrochloride is an orally active, potent and selective FLT3 inhibitor. Quizartinib dihydrochloride inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib dihydrochloride inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib dihydrochloride can be used for the research of cancer .
|
-
-
- HY-103195
-
NKY80
2 Publications Verification
|
Adenylate Cyclase
|
Metabolic Disease
|
|
NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
|
-
-
- HY-108642B
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
-
- HY-119939
-
|
CHDI00390576
|
HDAC
|
Cancer
|
|
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
|
-
-
- HY-153450
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
|
-
-
- HY-163638
-
|
|
Epigenetic Reader Domain
Molecular Glues
E1/E2/E3 Enzyme
|
Cancer
|
|
BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
|
-
-
- HY-105064D
-
|
CP-597396 hydrochloride hydrate
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
|
-
-
- HY-D1341
-
|
|
Fluorescent Dye
|
Cancer
|
|
Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .
|
-
-
- HY-108532
-
|
|
RAR/RXR
|
Cancer
|
|
AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0 .
|
-
-
- HY-134194
-
KL201
2 Publications Verification
|
Cryptochrome
|
Metabolic Disease
|
|
KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .
|
-
-
- HY-108526
-
|
|
RAR/RXR
Autophagy
|
Others
|
|
AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
|
-
-
- HY-126145
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4 .
|
-
-
- HY-15280
-
|
|
PI3K
|
Inflammation/Immunology
|
|
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .
|
-
-
- HY-12828A
-
|
|
CDK
DYRK
|
Infection
Neurological Disease
|
|
KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM) .
|
-
-
- HY-128772
-
|
|
Sodium Channel
|
Neurological Disease
|
|
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity .
|
-
-
- HY-125838
-
|
|
JNK
|
Neurological Disease
|
|
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases .
|
-
-
- HY-P5174
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
|
-
-
- HY-13223A
-
|
CP 868596-26
|
Autophagy
PDGFR
FLT3
|
Cancer
|
|
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
-
- HY-W074537
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
P7-2104 is a selective CNS-penetrant PDE7A inhibitor with an IC50 of of 31 nM. P7-2104 exhibits selectivity over hERG channels and most CYP450 isoforms. P7-2104 can be used for PDE7-targeted PET neuroimaging, and for the research of neurodegenerative disorders .
|
-
-
- HY-111509
-
|
|
ROR
|
Inflammation/Immunology
|
|
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) .
|
-
-
- HY-112547
-
|
CRT0066051
|
PKD
|
Others
|
|
CRT5, a pyrazine benzamide, is a potent and selective inhibitor for all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). CRT5 decreases VEGF-induced endothelial migration, proliferation and tubulogenesis .
|
-
-
- HY-123825
-
-
-
- HY-119254A
-
|
|
Epigenetic Reader Domain
|
Metabolic Disease
|
|
trans-BAY-850 is the trans isomer of BAY-850 (HY-119254). BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
|
-
-
- HY-13223R
-
|
CP-868596 (Standard)
|
FLT3
PDGFR
Autophagy
Reference Standards
|
Cancer
|
|
Crenolanib (Standard) is the analytical standard of Crenolanib. This product is intended for research and analytical applications. Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
-
- HY-113957
-
|
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM .
|
-
- HY-103384
-
|
|
Casein Kinase
|
Cancer
|
|
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
|
-
- HY-150692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-P2261
-
STAD 2
1 Publications Verification
|
PKA
|
Infection
|
|
STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
|
-
- HY-163145
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
|
-
- HY-139177
-
|
|
PPAR
|
Cardiovascular Disease
|
|
PPARα agonist 2 (compound 4u) is a potent and selective PPARα agonist with an EC50 of 37 nM. PPARα agonist 2 exhibits >2,700-fold selectivity for PPARα over other PPAR isoforms. PPARα agonist 2 has the potential for retinal disorders research .
|
-
- HY-148742
-
|
|
RET
|
Cancer
|
|
RET-IN-21 (compound 5) is a selective RET V804M inhibitor with the IC50 of 0.02 μM. RET-IN-21 does not inhibit the wild type isoforms of RET or KDR. RET-IN-21 has antitumor activity .
|
-
- HY-126585S
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAICAR-d3 is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
|
-
- HY-131305
-
|
|
PKC
Apoptosis
|
Neurological Disease
|
|
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .
|
-
- HY-17464S1
-
-
- HY-P1219
-
|
β-TRTX-Cj1α
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
|
-
- HY-150595
-
|
|
HDAC
Microtubule/Tubulin
|
Cancer
|
|
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
|
-
- HY-109068A
-
|
INCB050465 hydrochloride; IBI-376 hydrochloride
|
PI3K
|
Cancer
|
|
Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies .
|
-
- HY-N1373A
-
|
(+)-Sophoridine
|
Apoptosis
|
Cancer
|
|
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
|
-
- HY-105402
-
|
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
T 162559 is a potent and selective inhibitor of the Na+/H+ exchanger isoform NHE1 with IC50 values of 0.96 nM. T 162559 does not affect Na+/HCO3- cotransport and Na+/Ca2+ exchange. T 162559 can be used for the research of cardiovascular disease .
|
-
- HY-162388
-
|
|
AAK1
|
Neurological Disease
|
|
TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity .
|
-
- HY-105064B
-
|
CP-597396 hydrochloride
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
|
-
- HY-105064DR
-
|
CP-597396 hydrochloride hydrate (Standard)
|
Reference Standards
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
Zoniporide (hydrochloride hydrate) (Standard) is the analytical standard of Zoniporide (hydrochloride hydrate). This product is intended for research and analytical applications. Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
|
-
- HY-101972A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
AZ-PFKFB3-67 quarterhydrate is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively .
|
-
- HY-162767
-
|
|
HSP
|
Neurological Disease
|
|
KUNG65 is a selective inhibitor of Grp94, with a target Kd of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms .
|
-
- HY-159568
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-22 is a highly selective inhibitor of human carbonic anhydrase (hCA) isoform XII (Ki=9.7 nM) with anticancer activity .
|
-
- HY-112286
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM .
|
-
- HY-158078
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 21 (Compound 5h) is a selective carbonic anhydrase (hCA IX) inhibitor, with a Ki of 15.1?nM, and is highly selective against other investigated isoform. Carbonic anhydrase inhibitor 21 can be used for anticancer research .
|
-
- HY-147220
-
|
Dex-Ox
|
Progesterone Receptor
|
Endocrinology
|
|
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms .
|
-
- HY-178352
-
|
|
Monoamine Oxidase
Reactive Oxygen Species (ROS)
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-49 is a selective and reversible MAO-B inhibitor (IC50 of 1 nM for human MAO-B). MAO-B-IN-49 shows much higher selectivity for MAO-B than for MAO-A (IC50 = 633.9 μM). MAO-B-IN-49 can reduce ROS production induced by Lipopolysaccharides (HY-D1056) (LPS) in HT22 cells. MAO-B-IN-49 demonstrates substantial neuroprotective properties and significantly improves motor dysfunction in MPTP (HY-W114750)-induced mouse models of Parkinson’s disease (PD). MAO-B-IN-49 can be used for the study of PD .
|
-
- HY-144639
-
-
- HY-156181
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
|
-
- HY-17464S
-
-
- HY-17464R
-
|
OPC 13013 (Standard)
|
Reference Standards
Phosphodiesterase (PDE)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Cilostazol (Standard) is the analytical standard of Cilostazol. This product is intended for research and analytical applications. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
|
-
- HY-13245B
-
|
(Rac)-INCB8761
|
CCR
|
Inflammation/Immunology
|
|
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
|
-
- HY-103683R
-
|
|
Reference Standards
AMPK
|
Metabolic Disease
|
|
PF-06409577 (Standard) is the analytical standard of PF-06409577. This product is intended for research and analytical applications. PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
|
-
- HY-168154
-
|
|
COMT
|
Cancer
|
|
COMT-IN-2 (compund 9) is the potent COMT inhibitor, showing selective inhibition of brain (IC50=24 nM) and liver (IC50=81 nM) MB-COMT compared to the liver S-COMT (IC50=620 nM) isoform .
|
-
- HY-17464S2
-
-
- HY-150694
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
|
-
- HY-115917
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
NOS-IN-3 (Compound 9a) is a potent, selective, imidamide derived NOS inhibitor with an IC50 against iNOS of 4.6 μM, without inhibiting eNOS. NOS-IN-3 has little toxicity and can be studied in the research of inducible isoform involved diseases, such as septic shock .
|
-
- HY-12866R
-
|
LOXO-101 (Standard); ARRY-470 (Standard)
|
Reference Standards
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-13802R
-
|
GK 01140 (Standard)
|
IKK
Reference Standards
|
Cancer
|
|
SC-514 (Standard) is the analytical standard of SC-514. This product is intended for research and analytical applications. SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
|
-
- HY-158370
-
|
|
Casein Kinase
|
Cancer
|
|
CK2-IN-11 (32) is an allosteric CK2 inhibitor, with high selectivity for CK2 with IC50 values of 19.3 nM and 15.6 nM for the CK2α2β2 and the CK2α′2β2 isoforms, respectively .
|
-
- HY-108642A
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-132299
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation .
|
-
- HY-12866AR
-
|
LOXO-101 sulfate (Standard); ARRY-470 sulfate (Standard)
|
Trk Receptor
Apoptosis
Reference Standards
|
Cancer
|
|
Larotrectinib sulfate (Standard) is the analytical standard of Larotrectinib sulfate. This product is intended for research and analytical applications. Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-101972R
-
|
|
Phosphatase
Reference Standards
Bcl-2 Family
|
Neurological Disease
Metabolic Disease
|
|
AZ-PFKFB3-67 (Standard) is the analytical standard of AZ-PFKFB3-67 (HY-101972). This product is intended for research and analytical applications. AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity .
|
-
- HY-185359
-
|
|
HDAC
|
Others
|
|
HDAC6-IN-78 (Example 48) is a selective HDAC6 inhibitor with an IC50 of 24 nM. HDAC6-IN-78 shows no activity against other HDAC isoforms .
|
-
- HY-183320
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-81 is a potent selective HDAC6 inhibitor with an IC50 of 1 nM. HDAC6-IN-81 exhibits selectivity over class I HDAC isoforms (HDAC1/2/3/8). HDAC6-IN-81 can be used for the research of cancer .
|
-
- HY-17464S3
-
|
OPC 13013-d6
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
Cancer
|
|
Cilostazol-d6 (OPC 13013-d6) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
|
-
- HY-15245R
-
|
|
PI3K
|
Cancer
|
|
GSK2636771 (Standard) is the analytical standard of GSK2636771. This product is intended for research and analytical applications. GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
- HY-108532R
-
|
|
Reference Standards
RAR/RXR
|
Cancer
|
|
AC-261066 (Standard) is the analytical standard of AC-261066 (HY-108532). This product is intended for research and analytical applications. AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0 .
|
-
- HY-108318R
-
|
KIN 001-51 (Standard)
|
Reference Standards
Src
|
Cardiovascular Disease
Inflammation/Immunology
|
|
RK-24466 (Standard) is the analytical standard of RK-24466 (HY-108318). This product is intended for research and analytical applications. RK-24466 (KiN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.
|
-
- HY-109068AR
-
|
INCB050465 hydrochloride (Standard); IBI-376 hydrochloride (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Parsaclisib hydrochloride (Standard) is the analytical standard of Parsaclisib (hydrochloride) (HY-109068A). This product is intended for research and analytical applications. Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies .
|
-
- HY-109068R
-
|
INCB050465 (Standard); IBI-376 (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Parsaclisib (Standard) is the analytical standard of Parsaclisib (HY-109068). This product is intended for research and analytical applications. Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies .
|
-
- HY-11010A
-
|
|
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
AS601245 TFA is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 TFA exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
|
-
- HY-135746
-
-
- HY-107385R
-
|
ONO-9302 (Standard); SKF105657 (Standard)
|
Reference Standards
5 alpha Reductase
|
Cancer
|
|
Epristeride (Standard) is the analytical standard of Epristeride. This product is intended for research and analytical applications. Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
|
-
- HY-N2574
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
- HY-180824
-
|
|
p38 MAPK
|
Neurological Disease
|
|
P38-α MAPK-IN-11 (Compound 4C) is a selective inhibitor of P38α MAPK that can cross the blood-brain barrier with an IC50 value of 43 nM. P38-α MAPK-IN-11 has extremely low inhibitory activity against other MAPK subtypes, namely p38β, p38γ, and p38δ, with IC50 values of > 100 nM, > 100 nM, and 48.6 mM respectively. P38-α MAPK-IN-11 exhibits outstanding neuroprotective effects and anti-neuroinflammatory effects in Alzheimer's disease-like rat models. P38-α MAPK-IN-11 can be used for the study of Alzheimer's disease .
|
-
- HY-136735
-
|
|
IRE1
|
Neurological Disease
Cancer
|
|
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-108539A
-
|
|
Ras
|
Metabolic Disease
|
|
(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4 .
|
-
- HY-137295
-
|
|
PKC
Apoptosis
|
Inflammation/Immunology
|
|
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
|
-
- HY-147828
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
|
-
- HY-147827
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
|
-
- HY-10405
-
|
Ro4402257; R1503
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
|
-
- HY-123976A
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities .
|
-
- HY-155063
-
|
|
HSP
Mitochondrial Metabolism
|
Cancer
|
|
TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1，a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94，and disrupts TRAP1 tetramer stability，induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS，disrupts the mitochondrial membrane potential，and enhances glycolysis metabolism .
|
-
- HY-179019
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
Caspase
|
Neurological Disease
Cancer
|
|
HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research .
|
-
- HY-123976
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities .
|
-
- HY-108043
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki of 0.49 and 0.75 nM and EC50 of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .
|
-
- HY-175843
-
|
|
ROCK
STAT
|
Cancer
|
|
ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research .
|
-
- HY-139135
-
|
|
NO Synthase
|
Others
|
|
Methyl-L-NIO (compound 2d) hydrochloride is a potential selective inhibitor (IC50: 70 μM) of dimethylarginine dimethylaminohydrolase hDDAH. Methyl-L-NIO also has inhibitory activity against NO synthase. The inhibition rates of Methyl-L-NIO on different isoforms of NO synthase at a concentration of 100 μM are 77% (nNOS), 20% (eNOS), and 72% (iNOS) respectively; the inhibition rates at a concentration of 1 mM are 100% (nNOS), 85% (eNOS), 100% (iNOS) .
|
-
- HY-163384
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
(S)-CE-123 is a potent, selective, and novel atypical dopamine transporter (DAT) inhibitor with an EC50 of 2.76 μM in uptake inhibition assays conducted in HEK293 cells stably expressing human isoforms of DAT. (S)-CE-123, a Modafinil analogue, is able to penetrate the blood–brain barrier. (S)-CE-123 improves cognitive and motivational processes in experimental animals .
|
-
- HY-139004
-
|
|
Casein Kinase
|
Neurological Disease
|
|
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases .
|
-
- HY-176733
-
|
|
HDAC
Free Fatty Acid Receptor
Microtubule/Tubulin
ERK
|
Neurological Disease
|
|
HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC50: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a GPR40 activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease .
|
-
- HY-155671
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively .
|
-
- HY-17356
-
|
|
PPAR
Cytochrome P450
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-124432
-
|
|
Aldose Reductase
|
Cancer
|
|
CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC50=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer .
|
-
- HY-15565
-
APD668
2 Publications Verification
|
GPR119
Cytochrome P450
Potassium Channel
|
Metabolic Disease
|
|
APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-13001R
-
|
AC220 (Standard)
|
Reference Standards
FLT3
Apoptosis
PDGFR
c-Kit
|
Cancer
|
|
Quizartinib (AC220; AC708) (Standard) is the analytical standard of Quizartinib (HY-13001). This product is intended for research and analytical applications. Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
|
-
- HY-100022A
-
|
eFT508 hydrochloride
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-13001S
-
|
AC220-d8
|
Isotope-Labeled Compounds
Apoptosis
FLT3
PDGFR
c-Kit
|
Cancer
|
|
Quizartinib (AC220; AC708)-d8 is deuterium labeled Quizartinib (HY-13001). Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
|
-
- HY-18071A
-
|
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-P2802B
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase, rice is a GH31 glycoside hydrolase in rice seeds, with high selectivity for α-1,4-glycosidic bonds. α-Glucosidase, rice can be inhibited by rice husk extracts (IC50 = 1.25 μg/mL) and steroidal components (IC50 = 1.83 μg/mL). α-Glucosidase, rice exists in two major isoforms, among which isoform II is more sensitive to inhibitors. α-Glucosidase, rice can directly bind to and degrade starch granules in rice seeds. α-Glucosidase, rice can form ONG2-I and ONG2-II via post-translational proteolysis. α-Glucosidase, rice can be used in type 2 diabetes research .
|
-
- HY-104036R
-
|
|
Reference Standards
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH-305 (Standard) is the analytical standard of IDH-305 (HY-104036). This product is intended for research and analytical applications. IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT)) .
|
-
- HY-175232
-
|
|
Nuclear Factor of activated T Cells (NFAT)
Endogenous Metabolite
|
Endocrinology
|
|
GL64 is a selective agonist of ADGRD1 (EC50 = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases .
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-
- HY-159584
-
|
|
iGluR
|
Neurological Disease
|
|
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
|
-
- HY-N2574R
-
|
|
Reference Standards
Glycosidase
|
Metabolic Disease
|
|
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
|
-
- HY-151385
-
|
|
JAK
STAT
IFNAR
Interleukin Related
|
Cancer
|
|
VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 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-10118
-
|
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively . Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation .
|
-
- HY-146727
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases .
|
-
- HY-100022
-
|
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-180214
-
|
|
HDAC
|
Cardiovascular Disease
Neurological Disease
|
|
HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
|
-
- 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-10405R
-
|
Ro4402257 (Standard); R1503 (Standard)
|
Reference Standards
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Pamapimod (Standard) is the analytical standard of Pamapimod. This product is intended for research and analytical applications. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
|
-
- HY-17356S
-
-
- HY-103195R
-
|
|
Reference Standards
Adenylate Cyclase
|
Metabolic Disease
|
|
NKY80 (Standard) is the analytical standard of NKY80 (HY-103195). This product is intended for research and analytical applications. NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
|
-
- HY-132231
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
|
-
- HY-178327
-
|
|
DGK
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
DGKα/ζ-IN-2 is a potent, orally active and selective dual DGKα/ζ inhibitor with IC50 values of 23 nM (DGKα) and 1.2 nM (DGKζ). DGKα/ζ-IN-2 exhibits selectivity over other DGK isoforms, such as DGKβ and DGKγ. DGKα/ζ-IN-2 shows robust and dose-dependent immune activation in the presence of antigen presentation in an OT-1 murine model. DGKα/ζ-IN-2 can be used for antitumor immunity .
|
-
- HY-108642BR
-
|
|
Reference Standards
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 dihydrochloride (Standard) is the analytical standard of AMG-548 (dihydrochloride) (HY-108642B). This product is intended for research and analytical applications. AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein Kinase 1 isoforms δ and ε .
|
-
- HY-157129
-
|
|
AMPK
|
Cardiovascular Disease
|
|
AMPK-α1β1γ1 activator 1 (M1) is an acyl glucuronide metabolite of Indole-3-carboxylic Acid-based AMPK activator. AMPK-α1β1γ1 activator 1 can selectively activated human β1 isoforms with an EC50 value of 38.1nM. AMPK-α1β1γ1 activator 1 can direct binding with human AMPK α1β1γ1 isoform. AMPK-α1β1γ1 activator 1 can be used for the research of diabetic nephropathy .
|
-
- HY-18071
-
BI-9627
3 Publications Verification
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
|
BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-148135
-
|
|
Carbonic Anhydrase
|
Neurological Disease
|
|
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy .
|
-
- HY-Q51222
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
ZINC110492 is a selective ligand of CS-ΔEx4 (a splicing isoform of citrate synthase (CS)). ZINC110492 does not bind to CS full-length (CS-FL). ZINC110492 inhibits colorectal cancer (CRC) cell growth in cells overexpressing CS-ΔEx4 with an IC50 of 7.840 µM. ZINC110492 significantly decreases both citrate and 2-hydroxyglutarate (2-HG) levels in the CS-ΔEx4-overexpressing SW1116 cells .
|
-
- HY-17356S2
-
-
- HY-17356S1
-
|
|
PPAR
Autophagy
Cytochrome P450
|
Cardiovascular Disease
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively .
|
-
- HY-10405S
-
|
|
Isotope-Labeled Compounds
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
|
-
- HY-181022
-
|
|
Casein Kinase
|
Cancer
|
|
BMS-135 is a potenr, selective and ATP-competitive casein kinase 2 (CK2) inhibitor with IC50 of 0.8 and 0.3 nM for CK2αandCK2α′ isoforms. BMS-135 can simulate the structure of ATP and bind to the active pocket of CK2, thereby inhibiting its serine/threonine phosphorylation function. BMS-135 can inhibit cells proliferation and shows anti-tumor effect. BMS-135 can be used for research of colon cancer .
|
-
- HY-W013268
-
|
(+)-N-3-Benzylnirvanol
|
Cytochrome P450
|
Metabolic Disease
|
|
(S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 .
|
-
- HY-175179
-
|
|
Epigenetic Reader Domain
E1/E2/E3 Enzyme
|
Cancer
|
|
LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells .
|
-
- HY-17356R
-
|
|
Reference Standards
PPAR
Cytochrome P450
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-135746S
-
-
- HY-U00237B
-
|
|
Adrenergic Receptor
|
Others
|
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-180526
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases .
|
-
- HY-178913
-
|
|
JAK
STAT
|
Inflammation/Immunology
|
|
Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC50 = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis .
|
-
- HY-W074975
-
|
5-Amino-1,3,4-thiadiazole-2-sulfonamide
|
Carbonic Anhydrase
|
Cancer
|
|
CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is a selective inhibitor of carbonic anhydrase B (HCA-B) and isoforms I, II, IV, and VII. CL 5343 has a Ki of 7.9 nM for hCA II. CL 5343 acts as a CA9 ligand to achieve targeted delivery of maytansine to the cell membrane of SKRC52 renal cancer cells. CL 5343 is useful in the development of therapeutics for diseases associated with CA overactivity, such as glaucoma, epilepsy, and cancer .
|
-
- HY-15565R
-
|
|
GPR119
Cytochrome P450
Potassium Channel
|
Metabolic Disease
|
|
APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
|
-
- HY-119298
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
AW-814141 is a selective and orally active p38 MAP kinase inhibitor. AW-814141 has an IC50 values of 100 nM and 158 nM for p38-α and β isoforms, respectively. AW-814141 can inhibit the production of TNF-α induced by LPS (HY-D1056). AW-814141 can inhibit paw edema in rats in a dose-dependent manner. AW-814141 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases such as rheumatoid arthritis .
|
-
- HY-18540
-
KT109
1 Publications Verification
|
MAGL
DAGL
|
Metabolic Disease
Inflammation/Immunology
|
|
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-Arachidonoylglycerol (HY-W011051), Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages .
|
-
- HY-12946
-
|
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- HY-17356G
-
|
|
Cytochrome P450
PPAR
Autophagy
|
Cardiovascular Disease
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
- HY-12513
-
|
LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
|
-
- HY-146223
-
|
|
Ras
p38 MAPK
PI3K
Apoptosis
|
Cancer
|
|
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
|
-
- HY-139088
-
|
|
Protein Arginine Deiminase
|
Neurological Disease
|
|
PAD3-IN-1 (compound 14b) is an inhibitor of protein arginine deiminase (PAD) and is more than 10-fold more selective for PAD3 than PAD 1, 2, and 4. The IC50 values of PAD3-IN-1 for PAD 1, 2, 3, and 4 are 120, 27.5, 4.5, and 30.5 μM, respectively. And PAD3 is a PAD isoform associated with neurodegenerative responses to spinal cord injury, and PAD3-IN-1 could be used to study PAD-related neurological diseases .
|
-
- HY-180803
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LH17, a Kaempferol (HY-14590) derivative, is a potent and selective PDE4 inhibitor (PDE4D2 IC50 = 73 nM, PDE4B2 IC50 = 190 nM). LH17 exhibits remarkable selectivity (>136-fold) against other PDE isoforms (PDE1B/2A/3A/5A/8A/9A/10A) (IC50 > 10000 nM), with the exception of PDE7A1 (IC50 = 300 nM). LH17 distinctly interacts with PDE4 M-pocket. LH17 demonstrates remarkable anti-fibrotic efficacy in both in vitro and in vivo models. LH17 can be used for idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-126969
-
|
|
PPAR
|
Metabolic Disease
|
|
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
|
-
- HY-100794
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
|
-
- HY-122026
-
|
PF-367
|
GSK-3
|
Neurological Disease
|
|
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively .
|
-
- HY-123869
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
GR127935 is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 can be used in neurological disease research .
|
-
- HY-12946A
-
|
|
Glucocorticoid Receptor
Cytochrome P450
HCV Protease
|
Infection
Inflammation/Immunology
|
|
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
|
-
- HY-B0822S1
-
|
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
|
|
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-151929
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-4 is a potent and BBB-permeable inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoforms JNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM) . JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability .
|
-
- HY-160469
-
|
|
Akt
PROTACs
|
Cancer
|
|
INY-05-040 is an AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 exhibits anti-cancer activity. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines. INY-05-040 can suppress AKT signaling and induces the stress mitogen-activated protein kinase (MAPK) c-Jun N-terminal kinase (JNK). INY-05-040 is effective for breast cancer lines with a low-baseline activation of stress MAPK pathway. INY-05-040 can be studied for anti-cancer research .
|
-
- HY-152226
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction .
|
-
- HY-147423
-
|
NBI-921352; XEN901
|
Sodium Channel
|
Neurological Disease
|
|
Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
|
-
- HY-173481
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
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- HY-159852
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PI3K
Ras
Akt
|
Cancer
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BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
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- HY-12491
-
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PI3K
Apoptosis
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Cancer
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PIK-C98 is a potent and selective PI3K inhibitor, with IC50s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma .
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- HY-146223A
-
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Ras
PI3K
p38 MAPK
Apoptosis
|
Cancer
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(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
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- HY-112608
-
|
|
PI3K
|
Cancer
|
|
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
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- HY-183309
-
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FXR
17β-HSD
|
Inflammation/Immunology
|
|
FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis .
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HY-L099
-
|
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2,296 compounds
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MCE Targeted Diversity Library contains 2,296 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.
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HY-L158
-
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6,080 compounds
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According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,080 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
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HY-L159
-
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2,056 compounds
|
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Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 2,056 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.
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HY-L083
-
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3,516 compounds
|
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Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 3,516 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
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| Cat. No. |
Product Name |
Type |
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- HY-17356G
-
|
|
Fluorescent Dye
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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| Cat. No. |
Product Name |
Type |
-
- HY-17356G
-
|
|
Biochemical Assay Reagents
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5174
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
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- HY-P2261
-
STAD 2
1 Publications Verification
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PKA
|
Infection
|
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STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
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- HY-P1219
-
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β-TRTX-Cj1α
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Sodium Channel
|
Neurological Disease
|
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Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-17356S
-
|
|
|
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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-
- HY-126585S
-
|
|
|
SAICAR-d3 is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
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-
- HY-17464S1
-
|
|
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Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
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-
-
- HY-B0822S1
-
|
|
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Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
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-
-
- HY-17464S
-
|
|
|
Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
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-
-
- HY-17464S2
-
|
|
|
Cilostazol-d2 (OPC 13013-d2) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
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-
-
- HY-13001S
-
|
|
|
Quizartinib (AC220; AC708)-d8 is deuterium labeled Quizartinib (HY-13001). Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
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-
-
- HY-17356S2
-
|
|
|
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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-
-
- HY-17356S1
-
|
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively .
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-
-
- HY-10405S
-
|
|
|
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
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-
-
- HY-17464S3
-
|
|
|
Cilostazol-d6 (OPC 13013-d6) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
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-
-
- HY-135746S
-
|
|
|
OR-1896-d3 is the deuterium labeled OR-1896 (HY-135746). OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-159584
-
|
|
|
Azide
|
|
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-16482
-
|
|
|
Cationic Lipids
|
|
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD) .
|
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-17356G
-
|
|
Cytochrome P450
PPAR
Autophagy
|
Cardiovascular Disease
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
|
-
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