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BSJ-05-037

Chemical Structure : BSJ-05-037

CAS No.: 2756388-01-7

BSJ-05-037 (ITK degrader BSJ-05-037)

Catalog No.: PC-20466Not For Human Use, Lab Use Only.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

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    Biological Activity

    BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.
    BSJ-05-037 induces potent degradation of ITK dependent on CRBN, neddylation, and the proteasome.
    BSJ-05-037 induces GATA-3 loss and decreases chemotherapy resistance in vitro.
    BSJ-05-037 disrupts TCR signaling, downregulates the Th2-associated transcription factor GATA-3, and can overcome chemotherapy resistance in TCL models in vivo.

    Physicochemical Properties

    M.Wt 1022.21
    Formula C51H59N9O10S2
    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-(5-((5-(4-acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenyl)thio)thiazol-2-yl)-4-(4-(7-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)heptyl)piperazin-1-yl)benzamide

    References

    1. Jiang B, et al. Cell Chem Biol. 2023 Mar 27:S2451-9456(23)00086-7.

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