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| | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Basic information |
| Product Name: | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester | | Synonyms: | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester;Methyl 2-(1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl)-1H-benzo[d]imidazole-5-carboxylate;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-6-carboxylate;R-10015,inhibit,R10015,Inhibitor,LIMKs,Reverse Transcriptase,LIM Kinase (LIMK),R 10015 | | CAS: | 2097938-51-5 | | MF: | C20H19ClN6O2 | | MW: | 410.86 | | EINECS: | | | Product Categories: | | | Mol File: | 2097938-51-5.mol | ![1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Structure](CAS/20200331/GIF/2097938-51-5.gif) |
| | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Chemical Properties |
| 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 |
| | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Usage And Synthesis |
| 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 |
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| | 1H-Benzimidazole-6-carboxylic acid, 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]-, methyl ester Preparation Products And Raw materials |
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