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CAS No.: 2070015-22-2

OSU-T315 Catalog No. CSN18951

Synonyms: ILK-IN-2

ILK-IN-2 is a ILK inhibitor.

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400-920-2911

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技术信息

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8741 mL
- 9.3705 mL
- 18.7411 mL
- 5 mM
- 0.3748 mL
- 1.8741 mL
- 3.7482 mL
- 10 mM
- 0.1874 mL
- 0.9371 mL
- 1.8741 mL

技术信息

CAS号

2070015-22-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H30F3N5O

运输

蓝冰

分子量

533.59

别名

ILK-IN-2

溶解度

DMSO	100.0 mg/mL (187.4 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (18.7 mM)

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