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CAS No.: 924473-59-6

T56-LIMKi Catalog No. CSN20446

Synonyms: T5601640

T 5601640 is a selective LIMK2 inhibitor which can inhibit cofilin phosphorylation in cells that overexpress LIMK2 but not LIMK1.

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技术信息

生物活性

描述LIM kinases (LIMKs) are important cell cytoskeleton regulators that play a prominent role in cancer manifestation and neuronal diseases. The LIMK family consists of two homologues, LIMK1 and LIMK2, which differ from one another in expression profile, intercellular localization, and function^[3]. T5601640 is a selective inhibitor of LIMK2 and efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC₅₀ values of 18.3, 7.4, 35.2 and 90 μM, respectively. T5601640 decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma^[3]. T5601640 (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1_−/−MEFs with an IC₅₀ of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50 μM T5601640 causes a statistically significant reduction in the number of cells exhibiting stress fibers^[4]. T5601640 can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T5601640 (60 mg/kg) shows a significant decrease in tumor volume compared to control^[3].
作用机制T5601640, as a potential LIMK2 inhibitor, occupies both the ATP-binding and the substrate-binding sites.
参考文献

[1] Rak R, Haklai R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48.
[2] Mashiach-Farkash E, Rak R, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.
[3] Rak R, Haklai R, Elad-Tzfadia G, Wolfson HJ, Carmeli S, Kloog Y. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48. doi: 10.18632/oncoscience.7. PMID: 25593987; PMCID: PMC4295757.
[4] Mashiach-Farkash E, Rak R, Elad-Sfadia G, Haklai R, Carmeli S, Kloog Y, Wolfson HJ. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize the actin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39. doi: 10.18632/oncotarget.525. PMID: 22776759; PMCID: PMC3442289.

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
- 2.5685 mL
- 12.8426 mL
- 25.6853 mL
- 5 mM
- 0.5137 mL
- 2.5685 mL
- 5.1371 mL
- 10 mM
- 0.2569 mL
- 1.2843 mL
- 2.5685 mL

技术信息

CAS号

924473-59-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H14F3N3O3

运输

蓝冰

分子量

389.33

别名

T5601640

溶解度

DMSO	76.0 mg/mL (195.2 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (7.7 mM)

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