Bioactivity | 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]. | ||||||||||||
Invitro | 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: | ||||||||||||
In Vivo | 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: | ||||||||||||
Name | R-10015 | ||||||||||||
CAS | 2097938-51-5 | ||||||||||||
Formula | C20H19ClN6O2 | ||||||||||||
Molar Mass | 410.86 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [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. |