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Chemical Structure| 2070015-22-2 同义名 : ILK-IN-2
CAS号 : 2070015-22-2
货号 : A623292
分子式 : C30H30F3N5O
纯度 : 99%+
分子量 : 533.587
MDL号 : MFCD29924730
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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].
实验方案
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
参考文献

[1]Lee SL, Hsu EC, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74.

[2]Lee SL, Hsu EC, Chou CC, Chuang HC, Bai LY, Kulp SK, Chen CS. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. doi: 10.1021/jm2007744. Epub 2011 Aug 24. PMID: 21823616; PMCID: PMC3182772.