T56-LIMKi-T5601640-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemET56-LIMKiCat. No.: HY-19352CAS No.: 924473-59-6Synonyms: T5601640分式: CHFNO分量: 389.33作靶點(diǎn): LIM Kinase (LIMK)作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 36 mg/mL

2、(92.47 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5685 mL 12.8426 mL 25.6852 mL5 mM 0.5137 mL 2.5685 mL 5.1370 mL10 mM 0.2569 mL 1.2843 mL 2.5685 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 T56-LIMKi選擇性的LIMK2抑制劑。抑制Panc-1細(xì)胞

3、長(zhǎng)的IC50值為35.2 M。IC50 & Target LIMK2體外研究T56-LIMKi efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC501/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEvalues of 18.3, 7.4, 35.2 and 90 M, respectively. T56-LIMKi decreases phosphorylated cofilin (p-cofilin)leve

4、ls and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, gliomaand schwannoma 1. It blocks the phosphorylation of cofilin which leads to actin severance and inhibition oftumor cell migration, tumor cell growth, and anchorage-independent colony formation in s

5、oft agar. T56-LIMKi(10-50 M) reduces p-cofilin in a dose-dependent manner in NF1/MEFs with an IC50 of 30 M. Notably,the inhibitor does not affect the amounts of total cofil. 50M T56-LIMKi causes a statistically significantreduction in the number of cells exhibiting stress fibers 2.體內(nèi)研究 T56-LIMKi can

6、 induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treatedwith T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control 1.PROTOCOLCell Assay T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo.

7、 Mice treatedwith T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: T56-LIMKi is dissolved in 0.5% carboxymethylcellulose solution. Mice are implanted wit

8、h xenograftedAdministration 1 Panc-1 cells. Treatment is started 7 days later. Mice in the two experimental groups are each treated with adaily oral non-toxic dose of T56-LIMKi (30 or 60 mg/kg in gavage) and mice in the control group receives onlythe vehicle (0.5% CMC) in the gavage 1.MCE has not in

9、dependently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Rak R, et al. Novel LIMK2 Inhibitor Blocks Panc-1 Tumor Growth in a mouse xenograft model. Oncoscience. 2014 Jan 1;1(1):39-48.eCollection 2014.2. Mashiach-Farkash E, et al. Computer-based identification of a novel LIMK1/2 inhibitor that synergizes with salirasib to destabilize theactin cytoskeleton. Oncotarget. 2012 Jun;3(6):629-39.McePdfHeightCaution: Product has not been fully validated fo