DCPR049-12 | Type I PRMTs inhibitor | Probechem Biochemicals

Chemical Structure : DCPR049-12

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DCPR049-12 (DCPR049_12)

货号: PC-28673Not For Human Use, Lab Use Only.

DCPR049_12 (DCPR049-12) is a potent, selective inhibitor of type I PRMTs with IC50 of 1.1 nM (PRMT1), 22 nM (PRMT3), 63 nM (PRMT4), 1.2 nM (PRMT6) and 1.8 nM (PRMT8), does not inhibit PRMT5.

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生物&药学活性

DCPR049_12 (DCPR049-12) is a potent, selective inhibitor of type I PRMTs with IC50 of 1.1 nM (PRMT1), 22 nM (PRMT3), 63 nM (PRMT4), 1.2 nM (PRMT6) and 1.8 nM (PRMT8), does not inhibit PRMT5.
DCPR049_12 shows minimal inhibitory effects on the other methyltransferases including 7 PKMTs (EZH2, DOT1L, G9a, MLL1, PRDM9, SMYD2, and SUV39H1), as well as DNA methyltransferases (DNMT1 and DNMT3A/3L) and histone acetyltransferase GCN5.
DCPR049_12 inhibits cancer cell proliferation against leukemia cell lines (KOPN-8, KMS11, MV4-11, THP-1, RS4.11, RCH-ACV, REH, and U937).
DCPR049_12 (0-15 uM) causes cell cycle arrest, apoptosis induction, and leukemogenic gene regulation in MV4-11 cells.

物理化学性质&存储条件

分子量	306.85
分子式	C16H19ClN2S
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	N1-(2-((2-chlorophenyl)thio)benzyl)-N1-methylethane-1,2-diamine

参考文献

1. Wang C, et al. J Med Chem. 2017 Nov 9;60(21):8888-8905.

DCPR049-12 (DCPR049_12)

生物&药学活性

物理化学性质&存储条件

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DCPR049-12 (DCPR049_12)

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