2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. Mps1/TTK-IN-1

Mps1/TTK-IN-1 (Compound cpd-5) 是 NMS-P715 (HY-12382) 的衍生物，是一种 Mps1 激酶抑制剂，其 IC50 值为 9.2 nM，Kd 值为 1.6 nM。Mps1/TTK-IN-1 特异性靶向 Mps1 激酶的 ATP 结合口袋。Mps1/TTK-IN-1 对 Mps1 耐药突变体 (C604Y、C604W) 保持抑制活性，其 IC50 值分别为 170 nM 和 19 nM，Kd 值为 471 and 349 nM。Mps1/TTK-IN-1 能够阻断 Mps1 介导的动粒蛋白 KNL1 的磷酸化，干扰纺锤体组装检查点功能，阻止染色体的正确分离，从而抑制肿瘤细胞的有丝分裂和增殖。

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Mps1/TTK-IN-1

Mps1/TTK-IN-1 Chemical Structure

CAS No. : 1202055-39-7

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Mps1/TTK-IN-1 相关抗体

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  • 生物活性

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生物活性

Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715 (HY-12382), is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells[1].

分子量

580.72

Formula

C33H40N8O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Mps1/TTK-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Mps1/TTK-IN-11202055-39-7Mps1Monopolar spindle 1Inhibitorinhibitorinhibit

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