R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1.
IC50&Target
human LIMK1
38 nM (IC50)
体外研究
R-10015 (100 μM; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.
R-10015 inhibits HIV-1 DNA synthesis, nuclear migration, and virion release.
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) .
Western Blot Analysis
Cell Line:
CEM-SS T cells
Concentration:
100 μM
Incubation Time:
0 hour,0.5 hour,1 hour,2 hours,4 hours
Result:
Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.
体内研究
R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.
Animal Model:
6-8 weeks female C3H/HeN mice
Dosage:
10 mg/kg
Administration:
Intraperitoneal injection
Result:
Displayed none indication of toxicity.
分子式
C20H19ClN6O2
分子量
410.86
CAS号
2097938-51-5
运输条件
Room temperature in continental US; may vary elsewhere.