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SJ432

Chemical Structure : SJ432

CAS No.: 2230677-55-9

SJ432 (SJ-432)

Catalog No.: PC-72187Not For Human Use, Lab Use Only.

SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.

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

    Biological Activity

    SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.
    SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).
    SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.
    SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.

    Physicochemical Properties

    M.Wt 371.444
    Formula C22H21N5O
    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

    4-[[(2S,4R)-1-Acetyl-1,2,3,4-tetrahydro-2-methyl-6-(1H-pyrazol-3-yl)-4-quinolinyl]amino]benzonitrile

    References

    1. P Jake Slavish, et al. Cancer Res. 2020 Sep 1;80(17):3507-3518.

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