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PRC1 inhibitor RB-3

Chemical Structure : PRC1 inhibitor RB-3

CAS No.: 2396639-11-3

PRC1 inhibitor RB-3 (RB-3)

Catalog No.: PC-38305Not For Human Use, Lab Use Only.

PRC1 inhibitor RB-3 (RB-3) is a small molecule PRC1 inhibitor that directly bind to RING1B-BMI1 (KD=2.8 uM), the heterodimeric complex constituting the E3 ligase activity of PRC1.

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    Biological Activity

    PRC1 inhibitor RB-3 (RB-3) is a small molecule PRC1 inhibitor that directly bind to RING1B-BMI1 (KD=2.8 uM), the heterodimeric complex constituting the E3 ligase activity of PRC1.
    RB-3 bind to RING1B by inducing the formation of a hydrophobic pocket in the RING domain.
    RB-3 decreases the global level of H2A ubiquitination (IC50=1.6 uM) and induces differentiation in leukemia cell lines and primary AML samples.
    RB-3 represents a valuable chemical tool to study PRC1 biology.

    Physicochemical Properties

    M.Wt 417.893
    Formula C24H20ClN3O2
    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

    1H-Pyrrole-2-carboxylic acid, 3-(5-chloro-1H-indol-4-yl)-5-(1H-indol-4-yl)-4-(1-methylethyl)-

    References

    1. Shukla S, et al. Nat Chem Biol. 2021 Jul;17(7):784-793.

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