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R-10015

  Cat. No.:  DC11706   Featured
Chemical Structure
2097938-51-5
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More than 5000 active chemicals with high quality for research!
Field of application
A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .
Cas No.: 2097938-51-5
Chemical Name: Methyl 2-(1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl) piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxylate
Synonyms: R 10015;R10015
SMILES: C(C1CCN(C2N=CN=C3NC=C(Cl)C3=2)CC1)1=NC2=CC(C(OC)=O)=CC=C2N1
Formula: C20H19ClN6O2
M.Wt: 410.86
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
Target: human LIMK1:38 nM (IC50)
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: 6-8 weeks female C3H/HeN mice[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection Result: Displayed none indication of toxicity.
In Vitro: 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.
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC11706 R-10015 A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .
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