mps1

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

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。

CFI-402257 是 Mps1/TTK 激酶的选择性抑制剂（Mps1 Ki = 0.09 nM；EC50 = 6.5 nM），可用于肝细胞癌疾病的研究。

BAY1217389 是一种有效的选择性单极纺锤体 1 (MPS1) 激酶抑制剂 ，IC50值小于10 nM。

AZ3146 是一种选择性 Mps1 抑制剂，IC50为 35 nM。

Empesertib (BAY 1161909) 是一种口服有效的Mps1抑制剂，IC50值小于1 nM，具有潜在的抗肿瘤活性。

MPI0479605 是一种选择性的，ATP 竞争性的 Mps1抑制剂，IC50值为 1.8 nM。

BOS-172722 是一种单极纺锤体 1 (MPS1) 检查点抑制剂，对MPS1 (1 mM ATP) 和P-MPS1 的IC50值分别为 11 nM 和 63 nM。它可研究多种乳腺癌。

NMS-P715 是一种 ATP 竞争性MPS1选择性抑制剂，IC50值为 182 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-8是一种Mps1抑制剂，可应用于各种肿瘤的研究。

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).

Mps1-IN-6（Compound 9）为一种高效Mps1抑制剂，具有6.4 nM的IC50值，并在乳腺癌细胞上展现出明显的抗增殖及抗肿瘤效果。

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。

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。

TC-Mps1-12 is an effective and selective inhibitor of monopolar spindle 1 (IC50: 6.4 nM) .

Mps1-IN-3 hydrochloride 是一种有效的、选择性的 Mps1 抑制剂 (IC50: 50 nM)。Mps1-IN-3 hydrochloride 对胶质母细胞瘤细胞的增殖表现出抑制作用，并在原位异种移植瘤模型中可有效地使胶质母细胞瘤对长春新碱敏感。

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。

CCT-271850 is an inhibitor of the spindle checkpoint function of Monospindle 1.

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.)

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。

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。

CCT251455 is an inhibitor of mitotic kinase monopolar spindle 1 (MPS1; IC50: 3 nM).

Rac-CCT-250863, a potent Nek2 inhibitor, exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.

Mps-BAY2b is a novel MPS1 inhibitor.