上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Mps1-IN-1 dihydrochloride
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-1 dihydrochloride Chemical Structure
CAS No. : 1883548-93-3
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| 生物活性 |
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells[1].
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| IC50 & Target[1] |
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Mps1
367 nM (IC50)
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Mps1
27 nM (Kd)
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ALK
21 nM (Kd)
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LTK
29 nM (Kd)
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PYK2
280 nM (Kd)
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FAK
440 nM (Kd)
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IGF1R
750 nM (Kd)
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INSR
470 μM (Kd)
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CLK1
1900 nM (Kd)
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ERK2
2900 nM (Kd)
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INSRR
1200 nM (Kd)
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TNK1
2600 nM (Kd)
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TNK2
3100 nM (Kd)
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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