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描述 | Integrin-linked kinase (ILK) mediates the phosphorylation of multiple signaling proteins, such as Akt at Ser-473, GSK3β and myosin light chain. ILK-IN-2 is an ILK inhibitor with an IC50 value of 0.6 μM. It showed high anti-proliferative potency in a panel of prostate and breast cancer cell lines with IC50 values ranging from 1 – 2.5 μM. On the contrary, the viability of normal prostate epithelial cells and mammary epithelial cells was not affected by ILK-IN-2 at the doses of 1 – 5 μM. In PC-3 and SKBR3 cell lines, ILK-IN-2 dose-dependently downregulated the expressions of YB-1, HER2, and EGFR at both protein and transcript levels. The overexpression of constitutively active-ILK, however, diminished the suppressive effect of ILK-IN-2 on these signaling effectors. ILK-IN-2 at 1 – 4 μM exhibited dose-dependent inhibitory effects on the phosphorylation of ERK1/2 and p38, but not JNK. Moreover, ILK-IN-2 at 1 – 4 μM induced apoptosis and autophagy in PC-3 cells after 24h of treatment. In an ectopic PC-3 tumor xenograft model, oral treatment of ILK-IN-2 (25 and 50 mg/kg, once daily) for 35 days significantly suppressed tumor growth relative to vehicle-treated controls. A dose-dependent inhibition of the phosphorylation of Ser-473-Akt, GSK3β and MLC was also observed in ILK-IN-2-treated mice[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.87mL 0.37mL 0.19mL |
9.37mL 1.87mL 0.94mL |
18.74mL 3.75mL 1.87mL |
CAS号 | 2070015-22-2 |
分子式 | C30H30F3N5O |
分子量 | 533.587 |
别名 | ILK-IN-2 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 250 mg/mL(468.53 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |