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T56-LIMKi

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Chemical Structure| 924473-59-6 同义名 : T 5601640;T56-LIM Kinase Inhibito
CAS号 : 924473-59-6
货号 : A144833
分子式 : C19H14F3N3O3
纯度 : 99%+
分子量 : 389.328
MDL号 : MFCD08495674
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(269.7 mM)，配合低频超声助溶，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 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.69mL

5.14mL

2.57mL
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.