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KH-4-43

Chemical Structure : KH-4-43

CAS No.: 2813310-07-3

KH-4-43 (E3 CRL4 inhibitor)

Catalog No.: PC-72548Not For Human Use, Lab Use Only.

KH-4-43 is a small moelcule E3 CRL4 inhibitor and exhibits antitumor potential, directly and selectively binds to the purified E3 ROC1-CUL4A CTD complex with Kd of 83 nM.

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

    Biological Activity

    KH-4-43 is a small moelcule E3 CRL4 inhibitor and exhibits antitumor potential, directly and selectively binds to the purified E3 ROC1-CUL4A CTD complex with Kd of 83 nM.
    KH-4-43 weakly binds to the purified, highly related E3 ROC1-CUL1 CTD complex with Kd of 9.4 uM, >100-fold less potent than ROC1-CUL4A CTD, showed little effect on Ub thiol ester formation with E1/E2 Cdc34.
    KH-4-43 inhibited the ubiquitination of CK1α by CRL4CRBN in vitro. Treatment of cells with KH-4-43 caused accumulation of the E3 CRL4 substrate CDT1.
    KH-4-43 inhibited cell viability against a panel of tumor lines, NB-4, MV4-11, OVCAR-3, and CAPAN-2 cell with IC50 of 1.8, 3.0, 3.9, and 4.8 uM, respectively.
    KH-4-43 suppress the growth of human tumor xenografts in mice.

    Physicochemical Properties

    M.Wt 422.744
    Formula C19H10ClF3N2O4
    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

    3-[1-(4-Chlorophenyl)-1H-pyrazol-4-yl]-7,8-dihydroxy-2-(trifluoromethyl)-4H-1-benzopyran-4-one

    References

    1. Kenneth Wu, et al. Proc Natl Acad Sci U S A. 2021 Feb 23;118(8):e2007328118.

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