BBDDL2059 | EZH2 inhibitor | Probechem Biochemicals

Chemical Structure : BBDDL2059

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BBDDL2059 (BBDDL 2059)

货号: PC-20858Not For Human Use, Lab Use Only.

BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2.

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生物&药学活性

BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2.
BBDDL2059 demonstrates excellent cellular potency with IC50 values of 0.064 and 0.022 μM in inhibition of KARPAS-422 and Pfeiffer cell growth, respectively.
BBDDL2059 shows no significant inhibitionagainst a panel of 10 methyltransferases at 10 uM, including DNA methyltransferase DNMT1, arginine methyltransferases (PRMT1, PRMT4, and PRMT5), and protein lysine methyltransferases (G9a, GLP, MLL1, and MLL4).
BBDDL2059 (0.05-1 uM) effectively reduced the H2K27me3 mark in a concentration- and time- dependent manner but had no effect on the total H3 and EZH2 in KARPAS-422 cells.

物理化学性质&存储条件

分子量	512.67
分子式	C27H36N4O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(acrylamidomethyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzamide

参考文献

1. Yi Zhang, et al. J Med Chem. 2023 Jun 8;66(11):7629-7644.

BBDDL2059 (BBDDL 2059)

生物&药学活性

物理化学性质&存储条件

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BBDDL2059 (BBDDL 2059)

生物&药学活性

物理化学性质&存储条件

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