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NVP-HDM201 (HDM201) is a potent and highly specific MDM-2/p53 inhibitor currently under phase I clinical trial. HDM2 inhibitor HDM201 inhibits the binding of the HDM2 protein ...
TAK-659 is an inhibitor of spleen tyrosine kinase (syk), with potential anti-inflammatory, immunomodulating, and antineoplastic activities. It is in phase I/II clinical trials for ...
Mitapivat is a potent human R-type pyruvate kinase (PKR) inhibitor; also shows potency for mutant PKR including R510Q PKR, R532W PKR, T384W PKR etc.
AG-881 is an oral inhibitor of mutated isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2). In preclinical studies, AG-881 demonstrated the ability to penetrate the blood-brain barrier.
ML-7 hydrochloride is a MLCK inhibitor. ML-7 inhibits smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM.
EPZ004777 is a potent, selective inhibitor of DOT1L. Treatment of mixed lineage leukemia (MLL) cells with EPZ004777 selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes.
Alvocidib (Flavopiridol) hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7.
BAY 1895344 is a potent and selective ATR inhibitor, which shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy ...
TPX-0005 is a potent ALK/ROS1/TRK inhibitor with a rigid three-dimensional macrocyclic structure and a much smaller size (MW <370) than current ALK/ROS1/TRK inhibitors.
MK-4827 R-enantiomer is the R form of MK-4827(Niraparib), which is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM and used for the maintenance treatment ...
BMS-986020 (AM-152) is a LPA1 antagonist. It is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor ...
GDC-0152 is a potent inhibitor of IAPs which binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with Ki values of 28, 14, 17, and 43 nM, respectively.
LCL161 is a n orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins.
Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, with IC50 of 0.4 nM and 0.9 nM for Met and KDR, less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and has little activity to FGFR1 and EGFR.
PAC-1 (Procaspase activating compound 1) selectively induces apoptosis, or cell suicide, in cancerous cells. PAC-1 has shown good results in mouse models ...
Regorafenib monohydrate is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
AZD-9291 (Mereletinib) mesylate is a third generation irreversible EGFR tyrosine kinase inhibitor with selectivity against mutant versus wild-type forms of EGFR ...
Ansamitocin P 3' (Antibiotic C 15003P3'; Maytansinol butyrate) exhibits antitumour activity, is an antibody drug conjugate cytotoxin. It showed potent cytotoxicity against the human solid tumor cell lines A-549, HT-29.
Epirubicin (hydrochloride) is a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibiting Topoisomerase.
Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and induces microtubule disassembly in vitro. It is useful for preparing cell-binding/maytansinoid agent complexes.
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