R-10015 - LIMK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemER-10015Cat. No.: HY-120097CAS No.: 2097938-51-5分式: CHClNO分量: 410.86作靶點(diǎn): LIM Kinase (LIMK)作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62.5 mg/mL (152.12 mM;

2、Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.06 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.06 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 R-10015

3、種于 HIV 感染的譜抗病毒化合物， 效選擇性的 LIMK 抑制劑，通過(guò)結(jié)合 ATP 結(jié)合袋阻斷LIMK，抑制 LIMK1 的 IC50 值為 38 nM 1。IC50 & Target human LIMK138 nM (IC50)體外研究 R-10015 (100 M; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS Tcells 1.R-10015 inhibits HIV-1 DNA synthesis, nuclear migration, and v

4、irion release 1.R-10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV),Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1) 1.Western Blot Analysis 1Cell Line: CEM-SS T cellsConcentration: 100 MIncubation Time: 0 hour,0.5 hour,

5、1 hour,2 hours,4 hoursResult: Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.體內(nèi)研究 R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-termuse of LIMK inhibitors to block viral infections 1.Animal Model:

6、 6-8 weeks female C3H/HeN mice 1Dosage: 10 mg/kgAdministration: Intraperitoneal injectionResult: Displayed none indication of toxicity.REFERENCES1. Yi F, et al. Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1. J Virol. 2017 Jun 9;91(13). pii:e02418-16.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40