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HDAC1/2-IN-2

Chemical Structure : HDAC1/2-IN-2

CAS No.: 937727-03-2

HDAC1/2-IN-2

Catalog No.: PC-61915Not For Human Use, Lab Use Only.

HDAC1/2-IN-2 is a potent, selective HDAC1 and HDAC2 inhibitor with IC50 of 6 nM and 45 nM, respectively.

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    Biological Activity

    HDAC1/2-IN-2 is a potent, selective HDAC1 and HDAC2 inhibitor with IC50 of 6 nM and 45 nM, respectively.
    HDAC1/2-IN-2 displays highly selectivity over HDAC3 (IC50=7.0 μM), HDAC8 and 11 (IC50=20-25 uM) and no activity on HDACs 4-7.
    HDAC1/2-IN-2 increases lysine 5 of histone H2B (H2BK5) in HCT116 colon carcinoma cells with IC50 of 400 nM, inhibited the cell growth with GI50 of 97 nM.
    HDAC1/2-IN-2 exhibits tumor growth inhibition in HCT116 xenograft mice.

    Physicochemical Properties

    M.Wt 449.529
    Formula C23H23N5O3S
    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

    N-(2-amino-5-(thiophen-2-yl)phenyl)-6-(2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-8-yl)nicotinamide

    References

    1. Hamblett CL, et al. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5300-9.

    2. Methot JL, et al. ACS Med Chem Lett. 2014 Jan 2;5(4):340-5.

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