1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester

1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  R-10015 is a potent and selective LIM domain kinase (LIMK) inhibitor with IC50 of 38 nM for human LIMK1. It binds to the ATP-binding pocket and acts as a broad-spectrum antiviral compound for HIV infection.

• in vitro

  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) .< br/>

  Western Blot Analysis

  < td class="col1"> Result:

  Cell Line:	CEM-SS T cells
  Concentration:	100 μM
  Incubation Time:	0 hour,0.5 hour,1 hour,2 hours,4 hours
  Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.

• in vivo

  R-10015 (10 mg/kg; ip) displays no indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.
  

  < p>

  < /tr>

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

• target

  Target	Value
  hLIMK1 (Cell-free assay)	38 nM

1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(41)Suppliers