| Identification | Back Directory | [Name]
1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester | [CAS]
2097938-51-5 | [Synonyms]
methyl 2-(1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl)-1H-benzo[d]imidazole-6-carboxylate
Methyl 2-(1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxylate
1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester | [Molecular Formula]
C20H19ClN6O2 | [MDL Number]
MFCD32067935 | [MOL File]
2097938-51-5.mol | [Molecular Weight]
410.86 |
| Chemical Properties | Back Directory | [density ]
1.465±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 62.5 mg/mL (152.12 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.68±0.10(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
R-10015 is a potent and selective LIM domain kinase (LIMK) inhibitor with IC50 of 38 nM for human LIMK1. It binds to the ATP-binding pocket and acts as a broad-spectrum antiviral compound for HIV infection. | [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) .< br/> 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 | < td class="col1"> Result: | Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells. | | [in vivo]
R-10015 (10 mg/kg; ip) displays no indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.
< p> | Animal Model: | 6-8 weeks female C3H/HeN mice | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection | | Result: | Displayed none indication of toxicity. | < /tr> | [target]
| Target | Value | hLIMK1
(Cell-free assay) | 38 nM |
| [IC 50]
human LIMK1: 38 nM (IC50) | [storage]
Store at -20°C | [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. DOI:10.1128/JVI.02418-16 |
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
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