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  • IC261
    • SU-5607
    货号: abs817535
    CAS号: 186611-52-9
    分子式: C18H17NO4
    分子量: 311.33
    产品说明书
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    货号-规格 货期 价格 数量
    abs817535-2mg 1-2周 ¥689.00
    - +
    abs817535-5mg 1-2周 ¥931.00
    - +
    abs817535-10mg 1-2周 ¥1397.00
    - +
    abs817535-50mg 1-2周 ¥4997.00
    - +
    大包装询价
    产品描述
    描述

    IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

    纯度
    98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    SU-5607
    可溶性/溶解性
    DMSO:62mg/ml(199.15 mM)
    生物活性
    靶点
    Casein Kinase
    In vitro(体外研究)
    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively. IC261 is less active on PKA, p34cdc2, and p55fyn (IC50s > 100 μM). IC261 induces mitotic arrest, spindle defects and centrosome amplification in AC1-M88 cells. IC261 (1 μM) increases G2/M cells after 12 h, and causes cell death at 24 h in AC1-M88 cells. IC261 (1 μM) also induces apoptosis in the extravillous trophoblast hybrid cells. IC261 (1.25 μM) suppresses the proliferation of several pancreatic tumour cell lines, including ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1 and PancTu-2 cells. IC261 (1.25 μM) specifically enhances CD95-mediated apoptosis of pancreatic tumour cells.
    In vivo(体内研究)
    IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/∊, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice.
    参考文献
    参考文献
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    • 实验方法 实验条件
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