R-10015

Research use only, not for human use.

R-10015 is a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket(IC50 of 38 nM for human LIMK1),and a broad-spectrum antiviral compound for HIV infection.R10015 as a lead compound that blocks LIMK activity by binding to the ATP-binding pocket.?

R-10015 is a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket(IC50 of 38 nM for human LIMK1),and a broad-spectrum antiviral compound for HIV infection.R10015 as a lead compound that blocks LIMK activity by binding to the ATP-binding pocket.?R10015 specifically blocks viral DNA synthesis, nuclear migration, and virion release.?In addition, R10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1), suggesting that LIMK inhibitors could be developed as a new class of broad-spectrum antiviral drugs.

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.

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.

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Cell Cycle/DNA Damage

LIM Kinase (LIMK)

human LIMK1

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2097938-51-5

410.86

C20H19ClN6O2

>98% (HPLC)

DMSO:62.5 mg/mL (152.12 mM; Need ultrasonic)

COC(=O)c1ccc2[nH]c(nc2c1)C1CCN(CC1)c1ncnc2[nH]cc(Cl)c12

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(-20℃)

With Ice Pack

≥ 2 years