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MKK7-COV-3

Chemical Structure : MKK7-COV-3

CAS No.: 2283355-54-2

MKK7-COV-3 (MKK7 Covalent inhibitor 3)

Catalog No.: PC-35803Not For Human Use, Lab Use Only.

MKK7-COV-3 (MKK7 Covalent inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM).

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    Biological Activity

    MKK7-COV-3 (MKK7 Covalent inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM).
    MKK7-COV-3 shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without effect on p-ERK levels at 10 uM.
    MKK7-COV-3 displays remarkable selectivity against a kinome panel of 76 kinases, with very few kinases inhibited by more than 75% at 1 uM: Aurora kinase B, LRRK2, and MKK4, as well as FLT3。
    MKK7-COV-3 inhibits 60% of the CD86+ response in primary mouse B cells in response to LPS stimulation (10 μM, 2 hr pre-incubation).

    Physicochemical Properties

    M.Wt 277.327
    Formula C17H15N3O
    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-(3-(6-methyl-1H-indazol-3-yl)phenyl)acrylamide

    References

    1. Shraga A, et al. Cell Chem Biol. 2018 Oct 24. pii: S2451-9456(18)30344-1.

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