R-10015

CAS No. 2097938-51-5

R-10015( —— )

Catalog No. M22437 CAS No. 2097938-51-5

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.?

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    R-10015
  • Note
    Research use only, not for human use.
  • Brief Description
    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.?
  • Description
    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.
  • 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) . 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.
  • 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. Animal Model:6-8 weeks female C3H/HeN mice Dosage:10 mg/kg Administration:Intraperitoneal injection Result:Displayed none indication of toxicity.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    LIM Kinase (LIMK)
  • Recptor
    human LIMK1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2097938-51-5
  • Formula Weight
    410.86
  • Molecular Formula
    C20H19ClN6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:62.5 mg/mL (152.12 mM; Need ultrasonic)
  • SMILES
    COC(=O)c1ccc2[nH]c(nc2c1)C1CCN(CC1)c1ncnc2[nH]cc(Cl)c12
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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.
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