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MMK7 inhibitor 4a

Chemical Structure : MMK7 inhibitor 4a

CAS No.: 2328096-81-5

MMK7 inhibitor 4a

Catalog No.: PC-36064Not For Human Use, Lab Use Only.

MMK7 inhibitor 4a is a potent, sepecific, covalent inhibitor of MMK7 with IC50 of 10 nM, displays >800-fold selectivity over EGFR-WT and EGFR-L858R/T790M.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    MMK7 inhibitor 4a is a potent, sepecific, covalent inhibitor of MMK7 with IC50 of 10 nM, displays >800-fold selectivity over EGFR-WT and EGFR-L858R/T790M.
    MMK7 inhibitor 4a formed a covalent bond to Cys218 at the end of the hinge region of MMK7.
    MMK7 inhibitor 4a displayed an excellent selectivity profile at 1 uM against a panel of 320 kinases.
    MMK7 inhibitor 4a potently inhibits cellular JNK at 1 uM and completely inhibited its downstream effector c-Jun with no effect on the JNK-pathway.
    MMK7 inhibitor 4a is a valuable probe for further investigation to elucidate the function of MKK7 in cellular studies and in vivo.

    Physicochemical Properties

    M.Wt 457.50
    Formula C23H23N9O2
    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

    (R)-1-(3-(3-(1-(4-acetylphenyl)-1H-1,2,3-triazol-4-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one

    References

    1. Wolle P, et al. J Med Chem. 2019 Feb 15. doi: 10.1021/acs.jmedchem.9b00102.

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