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G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM.
LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.
FG-2216 (YM-311) is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
KN-93 free base is a CaMKII inhibitor. KN-93 suppresses ventricular arrhythmia induced by LQT2 without decreasing TDR. KN-93 inhibits androgen receptor activity ...
GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, and shows 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2, etc.
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment. AZD-5069 was shown to inhibit binding of radiolabeled CXCL8 to human CXCR2 with a pIC50 value of 9.1.
GSK-3326595 (EPZ015938) is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) that potently inhibits tumor growth in vitro and in vivo in animal models.
RO3280 (Ro5203280) is a potent and selective PLK 1 inhibitor with excellent in vitro cellular potency. RO3280 showed strong antitumor activity in xenograft mouse models.
M-3814 (MSC2490484A) is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities.
LGX-818 (Encorafenib) is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated...
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 ...
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