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RK-701

Chemical Structure : RK-701

CAS No.: 2648855-18-7

RK-701 (RK701)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 446.55
    Formula C26H30N4O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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