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AZD5904 is a potent orally bioavailable MPO inhibitor. In preclinical studies, AZD5904 inhibited the isolated MPO enzyme with an IC50 of 140 nM ...
CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK 9 kinases. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9...
BAY-1143572 is a potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I. BAY1143572 inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis.
VX-765 is an orally absorbed prodrug of VRT-043198, a potent and selective inhibitor of caspases belonging to the ICE/caspase-1 subfamily.
FF-10101 is a novel MS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) inhibitor. FF-10101 irreversibly binds to and inhibits the activity of FLT3.
AZD1390 is an ATM inhibitor. AZD1390 is a potent and selective ATM inhibitor with the ability to cross the blood-brain barrier suitable for the treatment of intracranial malignancies.
BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). BAY 1436032 is a double-digit nanomolar and selective pan-inhibitor...
LY3200882 is a novel, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 targets transforming growth factor-beta (TGFb), with potential antineoplastic activity.
AZD4635 (HTL1071) is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM. It reverses adenosine-mediated T-cell suppression and enhances anti-tumour immunity.
Lonafarnib (Sch66336) is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM.
PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO 2015033299 A1, compound example 4.
S3I-201 (NSC-74859) is a cell-permeable Stat3 inhibitor that binds to the Stat3-SH2 domain, prevents Stat3 phosphorylation/activation, dimerization, and DNA-binding.
ETC-159 (ETC-1922159) is a potent, selective and orally available PORCN inhibitor. ETC-159 blocks the secretion and activity of all Wnts. ETC-159 is remarkably effective in treating RSPO-translocation ...
AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM. AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50...
P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM. P005091 is a trisubstituted thiophene with dichlorophenylthio
P22077 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53...
Stattic is a potent inhibitor of STAT3, used for cancer treatment.Stattic inhibits STAT3 phosphorylation (Y705) in ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines...
EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against...
GNE-477 is a potent dual PI3K/mTOR inhibitor. Owing to the common association with oncogenic malignancies, the PI3K/AKT/mTOR signaling pathway is regarded as ...
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
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