T56-LIMKi
| CAS号 | 924473-59-6 | 货号 | BCP28984 |
| 中文名 | T56-LIMKi | ||
| 英文名 | T56-LIMKi | ||
| 中文别名 | |||
| 英文别名 | T56 LIMKi; T56LIMKi; T5601640; T56-LIM Kinase Inhibitor; | ||
| 分子式 | C19H14F3N3O3 | 分子量 | 389.33 |
| 生物活性 | T5601640, also known as T56-LIMKi, has high specific inhibitory activity for LIMK2 and shows little or no activity with LIMK1. T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation. It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively. Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | LIMK | ||
结构式
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