R10015


Catalog No. size PriceQuantity
M6991-2 2mg solid $110
M6991-10 10mg solid $447

Description

Cas:2097938-51-5

Product Information

R10015 is potent DNA synthesis inhibitor and virus inhibitor. 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.

 

Chemical Formula: C20H19ClN6O2

 

Exact Mass: 410.1258

 

Molecular Weight: 410.862

 

Elemental Analysis: C, 58.47; H, 4.66; Cl, 8.63; N, 20.46; O, 7.79

 

Synonym:

 

R-10015

R 10015

R10015

 

Chemical Name: 

Methyl 2-(1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl) piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxylate

 

InChi Key: 

MGRJCGXCUUCOQG-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C20H19ClN6O2/c1-29-20(28)12-2-3-14-15(8-12)26-17(25-14)11-4-6-27(7-5-11)19-16-13(21)9-22-18(16)23-10-24-19/h2-3,8-11H,4-7H2,1H3,(H,25,26)(H,22,23,24)

 

Smiles Code:

O=C(C1=CC=C2NC(C3CCN(C4=C5C(NC=C5Cl)=NC=N4)CC3)=NC2=C1)OC

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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) .

 

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.

 

 

References

 

  1. Yi F, Guo J, Dabbagh D, Spear M, He S, Kehn-Hall K, Fontenot J, Yin Y, Bibian M, Park CM, Zheng K, Park HJ, Soloveva V, Gharaibeh D, Retterer C, Zamani R, Pitt ML, Naughton J, Jiang Y, Shang H, Hakami RM, Ling B, Young JAT, Bavari S, Xu X, Feng Y, Wu Y. Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1. J Virol. 2017 Jun 9;91(13):e02418-16. doi: 10.1128/JVI.02418-16. PMID: 28381571; PMCID: PMC5469273.

 

Products are for research use only. Not for human use.

 

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