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BTB-1

CAS No. 86030-08-2

BTB-1 ( BTB1 | BTB 1 | BTB-1 )

产品货号. M19186 CAS No. 86030-08-2

BTB-1 是有丝分裂运动蛋白 Kif18A 的新型小分子抑制剂。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥462 有现货
10MG ¥648 有现货
25MG ¥1158 有现货
50MG ¥1960 有现货
100MG ¥2900 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    BTB-1
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    BTB-1 是有丝分裂运动蛋白 Kif18A 的新型小分子抑制剂。
  • 产品描述
    BTB-1 is a novel small molecule inhibitor of the mitotic motor protein Kif18A, which was identified by Catarinella et al. during a highthroughput screen against Kif18A?’s MT-stimulated ATPase activity, with an IC50 of 1.7?–1.9 M . It is selective within the kinesin subgroup of Kif4, Eg5, MKLP-1, MKLP-2, MPP1, CENP-E and MCAK, and during in vitro motility assays Kif18A?’s MT gliding ability was blocked by the addition of BTB-1 in a reversible manner. BTB-1 was found to be ATP competitive and MT uncompetitive, only inhibiting the ATPase activity of the MT-bound motor protein. BTB-1 could serve as a valuable tool in disentangling the nature of Kif18A?’s double functionality within mitosis and assessing for potential therapeutic utilities.
  • 体外实验
    BTB-1 blocks the motility of Kif18A in a reversible manner. BTB-1 inhibits Kif18A in an adenosine triphosphate (ATP)-competitive but microtubule-uncompetitive manner and slows down the progression of cells through mitosis. 100 μM BTB-1 does not significantly inhibit any of the other tested mitotic kinesins. BTB-1 competes with ATP for Kif18A binding only when the motor-protein is associated with its pseudosubstrate microtubules. HeLa cells treated with BTB-1 accumulate in mitosis in a dose-dependent manner. BTB-1 shows cell toxicity with an EC50 values of 35.8 μM. HeLa cells treated with 50 μM BTB-1 reveals severe defects in spindle morphology and chromosome alignment. Treatment with high concentrations of BTB-1 does not result in elongated spindles.
  • 体内实验
    ——
  • 同义词
    BTB1 | BTB 1 | BTB-1
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    mitotic kinesin Kif18A
  • 研究领域
    Cancer
  • 适应症
    ——

化学信息

  • CAS Number
    86030-08-2
  • 分子量
    297.71
  • 分子式
    C12H8ClNO4S
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 100 mg/mL; 335.90 mM
  • SMILES
    O=S(=O)(c1ccc(Cl)cc1[N+](=O)[O-])c1ccccc1
  • 化学全称
    4-chloro-2-nitro-1-(phenylsulfonyl)benzene

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Catarinella M., et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6.
产品手册
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