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RGFP963

Chemical Structure : RGFP963

CAS No.: 1396720-98-1

RGFP963 (RGFP 963)

Catalog No.: PC-20238Not For Human Use, Lab Use Only.

RGFP963 (RGFP 963) is a potent, selective class I HDAC inhibitor with IC50 of 1.51 uM, 0.75 and 0.096 uM for HDAC1, HDAC2, and HDAC3, respectively.

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    Biological Activity

    RGFP963 (RGFP 963) is a potent, selective class I HDAC inhibitor with IC50 of 1.51 uM, 0.75 and 0.096 uM for HDAC1, HDAC2, and HDAC3, respectively.
    RGFP963 weakly inhibits HDAC10 (IC50=10 uM), does not inhibit any other HDACs.
    RGFP963 is able to cross the blood brain barrier.
    RGFP963 (10 mg/kg) would be active during the consolidation window when administered after learning, exhibiting selective inhibition of HDAC1, HDAC2, and HDAC3 activity.
    RGFP963 enhances consolidation of cued fear extinction.
    RGFP963 induces largely distinct transcriptional profiles in the dorsal hippocampus of mature mice, enhances synaptic efficacy.
    RGFP963, but not RGFP966, rescues memory in a mouse model of Alzheimer's Disease.

    Physicochemical Properties

    M.Wt 344.42
    Formula C21H20N4O
    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

    (E)-N-(2-aminophenyl)-3-(1-cinnamyl-1H-pyrazol-4-yl)acrylamide

    References

    1. Bowers ME, et al. Learn Mem. 2015 Mar 16;22(4):225-31.

    2. Rumbaugh G, et al. Neuropsychopharmacology. 2015 Sep;40(10):2307-16.

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