R-10015

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[1].

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> LIM Kinase (LIMK)

human LIMK1:38 nM (IC50)

R-10015 (100 μM; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells[1]. R-10015 inhibits HIV-1 DNA synthesis, nuclear migration, and virion 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[1] 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.

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[1]. Animal Model: 6-8 weeks female C3H/HeN mice[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection Result: Displayed none indication of toxicity.

[1]. 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.