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CAS No. : 1883548-93-3
MCE 国际站:Mps1-IN-1 dihydrochloride
产品活性: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。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton
作用靶点:Mps1
In Vitro: Mps1-IN-1 dihydrochloride (2-10 μM; 96 hours) inhibits the proliferative capacity of HCT116 cells to 33% that of DMSO control.
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.
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.
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.
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.
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.
相关产品:TC-Mps1-12 | AZ3146 | Mps1-IN-1 | Mps1-IN-3 hydrochloride | NMS-P715 | Mps1-IN-4 | BOS-172722 | RMS-07 | Mps-BAY2a | MPI-0479605 | Empesertib | BAY1217389 | CCT251455 | Mps1-IN-5 | Mps1-IN-2 | Mps1-IN-6
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