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  • BX-912
    • BX-912; BX 912
    货号: abs810343
    CAS号: 702674-56-4
    分子式: C20H23BrN8O
    分子量: 471.35
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810343-5mg 1-2周 ¥1420.00
    - +
    abs810343-10mg 1-2周 ¥2557.00
    - +
    abs810343-50mg 1-2周 ¥6090.00
    - +
    abs810343-100mg 1-2周 ¥8272.00
    - +
    大包装询价
    产品描述
    描述

    BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    BX-912; BX 912
    外观
    Powder
    可溶性/溶解性
    DMSO :87 mg/mL (184.6 mM)

    Ethanol :87 mg/mL (184.6 mM)




    生物活性
    靶点
    PDK-1
    In vitro(体外研究)
    BX-912 also inhibits PKA, KDR, CDK2/cyclin E, Chck1, c-Kit, PKC, T-Fyn, Insulin receptor, and GSK3β with IC50s of 110 nM, 410 nM, 650 nM, 830 nM, 850 nM, 1.25 μM, 2.1 μM, 6.1 μM and 7.4 μM in kinase assays, respectively. BX-912 is identified in a coupled assay measuring PDK1- and PtdIns-3,4-P2-mediated Akt activation, which can detect inhibitors of PDK1, AKT2, or other steps critical for activation of AKT2. BX-912 potently inhibits PDK1 enzyme activity in a direct kinase assay format (IC50=26), although BX-912 fails to block preactivated AKT2 activity (IC50>10 μM). BX-912 binds to the ATP binding site of PDK1. The aminopyrimidine backbone of BX-912 adopts a similar orientation in the active site of PDK1. To examine the kinase selectivity of BX-912, its effects on the in vitro activity of 10 different Ser/Thr and tyrosine kinases are determined, including the related AGC kinases PKA and PKCα. BX-912 is 9-fold selective for PDK1 relative to PKA. BX-912 blocks PDK1 activity in PTEN-negative PC-3 cells. PTEN-negative PC-3 cells display constitutive activation of Akt which is reflected in high levels of the PDK1 product, phospho-Thr308-Akt.
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