RK-701 | G9a/GLP inhibitor | Probechem Biochemicals

Chemical Structure : RK-701

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RK-701 (RK701)

货号: PC-49612Not For Human Use, Lab Use Only.

RK-701 (RK701) is a potent, highly selective and reversible histone lysine methyltransferases G9a and G9a-like protein (GLP) inhibitor with IC50 of 23-27 nM and 53 nM, respectively.

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生物&药学活性

RK-701 (RK701) is a potent, highly selective and reversible histone lysine methyltransferases G9a and G9a-like protein (GLP) inhibitor with IC50 of 23-27 nM and 53 nM, respectively.
RK-701 is a histone H3 substrate-competitive inhibitor, displays >1000-fold selectivity against other methyltransferases.
In contrast to G9a inhibitors such as UNC0638, RK-701 shows essentially no cytotoxic effect on the viability of normal cells, including rat myoblast cell line H9c2 and HUDEP-2 cells.
RK-701 treatment (0.3 uM) for primary human CD34+ hematopoietic cells significantly increased γ-globin mRNA expression, the level of HbF expression, and the percentage of HbF-expressing cells without affecting cell viability or erythroid differentiation.
RK-701 induced fetal globin expression both in human erythroid cells and in mice.
RK-701 selectively upregulates BGLT3 by inhibiting the recruitment of two major γ-globin repressors in complex with G9a onto the BGLT3 gene locus through CHD4, a component of the NuRD complex.
RK-701 is a promising lead compound for the development of therapeutic agents for sickle cell disease (SCD), and a excellent chemical tool thus far for investigating the physiological roles of G9a both in vitro and in vivo.

物理化学性质&存储条件

分子量	446.55
分子式	C26H30N4O3
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	(S)-N-(1-((4-cyanophenyl)amino)-4-cyclopropyl-1-oxobutan-2-yl)-3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-2-carboxamide

参考文献

1. Shohei Takase, et al. Nat Commun. 2023 Jan 12;14(1):23.

RK-701 (RK701)

生物&药学活性

物理化学性质&存储条件

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RK-701 (RK701)

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物理化学性质&存储条件

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