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class I HDACs inhibitor JT86

Chemical Structure : class I HDACs inhibitor JT86

CAS No.: 2708136-83-6

class I HDACs inhibitor JT86

Catalog No.: PC-25167Not For Human Use, Lab Use Only.

class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.

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    Biological Activity

    class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.
    JT86 is much less active against the class IIa enzyme HDAC7.
    JT86 shows potent cytotoxic effect (IC50= 0.02-0.1 μM) across the five cancer cell lines with 15- to 23-fold increased potency over AR-42.
    JT86 induces concentration-dependent accumulation of acetylated histone H4 in MM96L melanoma cells, indicating inhibition of endogenous HDAC1.

    Physicochemical Properties

    M.Wt 390.44
    Formula C23H22N2O4
    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-(4-(Hydroxycarbamoyl)phenyl)-4-(naphthalen-2-yl)tetrahydro-2H-pyran-4-carboxamide

    References

    1. Jiahui Tng, et al. J Med Chem. 2020 Jun 11;63(11):5956-5971.

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