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。
| 生物活性 | Mps1-IN-1 dihydrochloride is a potent and ATP-competitiveMps1kinase inhibitor with anIC50of 367 nM. Mps1-IN-1 dihydrochloride inhibitMps1mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of bothcancerand ‘normal’ cells[1]. |
| IC50& Target[1] | Mps1 367 nM (IC50) | Mps1 27 nM (Kd) | ALK 21 nM (Kd) | LTK 29 nM (Kd) | PYK2 280 nM (Kd) | FAK 440 nM (Kd) | IGF1R 750 nM (Kd) | INSR 470 μM (Kd) | CLK1 1900 nM (Kd) | ERK2 2900 nM (Kd) | INSRR 1200 nM (Kd) | TNK1 2600 nM (Kd) | TNK2 3100 nM (Kd) | GAK 1100 nM (Kd) |
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体外研究
(In Vitro) | Mps1-IN-1 dihydrochloride (2-10 μM; 96 hours) inhibits the proliferative capacity of HCT116 cells to 33% that of DMSO control[1].
Mps1-IN-1 dihydrochloride (0.3-10 μM; 4 hours) induces bypass of a checkpoint-mediated mitotic arrest in a dose-dependent manner. Mps1-IN-1 dihydrochloride (10 μM) administration results in a dose-dependent decrease in the time spent in mitosis with nearly 100% U2OS cells initiating anaphase within 20 minutes[1].
Mps1-IN-1 dihydrochloride (0.5, 2, 10 μM) causes a dose-dependent reduction in hyper-phosphorylated Mps1 as demonstrated by a decrease in phosphorylation-induced mobility shift in UTRM10 LAP-Mps1 WT cells[1].
Mps1-IN-1 (5, 10 μM) arrested in mitosis using Nocodazole, results in a dose-dependent accumulation of 4c pHistone H3 negative cells in U2OS cells[1].
Acceleration of mitosis kinetics in Mps1-IN-1-treated cells had direct consequences on genomic stability with cells exhibiting significant signs of chromosome mis-alignment and chromosome mis-segregation[1].
Mps1-IN-1 dihydrochloride demonstrates greater than 1000-fold selectivity relative to the 352 member kinase panel with the major exceptions of Alk and Ltk[1].
Cell Proliferation Assay[1] | Cell Line: | HCT116 cells | | Concentration: | 2, 5, 10 μM | | Incubation Time: | 96 hours | | Result: | The proliferative capacity of HCT116 cells was reduced to 33% that of DMSO control. |
Cell Cycle Analysis[1] | Cell Line: | U2OS cells | | Concentration: | 0.3, 0.5, 1, 2, 5, 10 μM | | Incubation Time: | 4 hours | | Result: | Dropped levels of cyclin B protein, which accumulate in G2 and are sustained during an activated spindle checkpoint. |
Western Blot Analysis[1] | Cell Line: | Hela and U2OS cells | | Concentration: | 10 μM | | Incubation Time: | Pretreatment 1 hour before taxol and MG132 | | Result: | Caused a dose-dependent reduction in the phosphorylation status of Aurora B at threonine-232 (Thr232). |
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| 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. |
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