mps1-in-1

Mps1-IN-1 is a potent, selective and ATP-competitive inhibitor of Mps1 kinase (IC50 : 367 nM )

Mps1-IN-1 dihydrochloride 是一种有效的，ATP 竞争性 Mps1激酶抑制剂，IC50为 367 nM。Mps1-IN-1 dihydrochloride 抑制 Mps1有丝分裂激酶活性并沉默纺锤体组装检查点 (SAC) 功能。Mps1-IN-1 dihydrochloride 降低癌细胞和“正常”细胞的活力。

Mps1-IN-3 是一种有效的选择性 MPS1 激酶抑制剂，IC50值为 50 nM。

Mps1-IN-2 是一种 ATP 竞争性Mps1 Plk1选择性双重抑制剂，对 Mps1 的IC50和Kd 值分别为 145 和 12 nM，对 Plk1 的Kd 值为 61 nM。

PROTAC MPS1 degrader 2 (Compound 15) 作为一种有效的化合物，针对单极纺锤体1 (Mps1, TTK)、AURKA及AURKB展现出显著的降解活性，其DC50值分别为42.0 nM、2.1 nM和154.0 nM。此外，PROTACMPS1 degrader 1 主要被应用于急性髓系白血病的相关研究。

PROTAC MPS1 degrader 1 (Compound 19) 作为一种针对单极纺锤体 1 (Mps1, TTK)、AURKA及AURKB的高效降解剂，显示出其DC50值分别为17.7 nM、108.7 nM和570.3 nM。该化合物主要用于急性髓系白血病的相关研究。(Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

MPS1 TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1 TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1 TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol L) induced G2 M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)

Mps1-IN-4，一种针对Monopolar spindle 1 (Mps1)的选择性抑制剂，展现出抗增殖特性，适用于癌症领域的研究。

Mps1-IN-5是一种口服活性的Mps1抑制剂，其IC50为29 nM。它可诱导Apoptosis和G2 M期的胞周期停滞，展现出抗增殖和抗肿瘤活性，并通过抑制Mps1磷酸化来诱导DNA损伤。

RMS-07 是 Monopolar Spindle Kinase 1 (MPS1 TTK)的共价抑制剂，其 IC50值为 13.1 nM。RMS-07靶向激酶结构域的半胱氨酸。

Mps1-IN-6是一种有效的Mps1抑制剂，具有2.596 nM的IC50值，显示出抗增殖和抗癌活性。

CFI-402257 hydrochloride，一种具有高选择性和口服活性的TTK Mps1抑制剂，体外对TTK的IC50值为1.7 nM，显示出抗癌活性。

Mps1-IN-8是一种Mps1抑制剂，可应用于各种肿瘤的研究。