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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-GSK137
GSK137

Chemical Structure : GSK137

CAS No.: 2728727-91-9

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GSK137 (GSK-137)

货号: PC-38660Not For Human Use, Lab Use Only.

GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.
    GSK137 also displaced peptides from human nuclear receptor co-repressor 1 and BCL6 co-repressor corepressors, which bind in the same position as SMRT, both with a pIC50 of 7.6.
    GSK137 showed potency against mouse and rat BCL6 and SMRTwith pIC50 to be 7.8 and 7.6, respectively, inhibited binding of intracellular full-length human BCL6 to BCL6-binding domain of SMRT (residues 1292–1500) in live cells with pIC50 of 7.3.
    GSK137 antagonizes the binding of corepressors to BCL6 in cell-free and whole cell assays without causing loss of BCL6 protein.
    GSK137 caused little change in cell viability or proliferation in four BCL6-expressing B-cell lymphoma lines.
    GSK137 demonstrated reduction in specific antibody titers in response to immunization with T-dependent antigens at drug levels consistent with robust engagement with the BCL6 BTB-POZ domain target in vivo.

    物理化学性质&存储条件

    分子量 374.423
    分子式 C21H19FN6
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    5-((5S,7R)-3-fluoro-7-(2-methylpyridin-3-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-5-yl)quinolin-2-amine

    参考文献

    1. Andrew C Pearce, et al. J Biol Chem. 2021 Aug;297(2):100928.

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