R-10015

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

R-10015 是一种有效的选择性 LIM 结构域激酶 (LIMK) 抑制剂，可与 ATP 结合袋结合（人 LIMK1 的 IC50 为 38 nM），是一种治疗 HIV 感染的广谱抗病毒化合物。R10015 作为先导化合物通过与 ATP 结合口袋结合来阻断 LIMK 活性。

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