EPZ015666 (GSK3235025) --- PRMT5 Inhibitor

Overview
Catalog #	bs-60254c-2-mg-solid
Product Name	EPZ015666 (GSK3235025) --- PRMT5 Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 383.44 Formula: C20 H25 N5 O3 CAS Number: 1616391-65-1 InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N InChi: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1 Smiles: O[C@@H](CNC(=O)C1C=C(NC2COC2)N=CN=1)CN1CCC2=CC=CC=C2C1 Purity: 98.0 Solubility: DMSO and EtOH up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	EPZ015666, also known as GSK3235025, is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.