R10015

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.

Product information

CAS Number: 2097938-51-5

Molecular Weight: 410.86

Formula: C20H19ClN6O2

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

Smiles: COC(=O)C1C=C2N=C(NC2=CC=1)C1CCN(CC1)C1N=CN=C2NC=C(Cl)C=12

InChiKey: MGRJCGXCUUCOQG-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

R10015 (100 μM; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells. R10015 inhibits HIV-1 DNA synthesis, nuclear migration, and virion release. 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) .

In Vivo:

R10015 (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.