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178506 ERK Kinase Kinase 5 Inhibitor - CAS 1005775-56-3 - Calbiochem

178506
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178506-10MGCN
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable imidazopyridine compound that acts as a potent, ATP-binding site-targeting ASK1/MEKK5-selective inhibitor (IC50 = 14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6), while exhibiting much reduced or no activity toward a panel of 195 other kinases. Shown to inhibit STZ- (1 mM; Cat. No. 572201) induced JNK and p38 phosphorylation in INS-1 pancreatic β cells (IC50 <300 nM) and be orally available in rats in vivo.
      Catalogue Number178506
      Brand Family Calbiochem®
      SynonymsApoptosis Signal-Regulating Kinase 1 Inhibitor, ASK-1 Inhibitor, MAP Kinase Kinase Kinase 5 Inhibitor, MAP3K5 Inhibitor, MAPKKK5 Inhibitor, MEKK5 Inhibitor, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-tert-butylbenzamide, 2HCl, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-(2-methyl-2-propanyl)benzamide, 2HCl, 4-tert-Butyl-N-(6-(1H-imidazol-1-yl)imidazo(1,2-a)pyridin-2-yl)benzamide, 2HCl
      References
      ReferencesTerao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.
      Product Information
      CAS number1005775-56-3
      FormWhite powder
      Hill FormulaC₂₁H₂₁N₅O • 2HCl
      Chemical formulaC₂₁H₂₁N₅O • 2HCl
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetASK1/MEKK5
      Primary Target IC<sub>50</sub>14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      참고문헌 보기
      Terao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision12-September-2013 JSW
      SynonymsApoptosis Signal-Regulating Kinase 1 Inhibitor, ASK-1 Inhibitor, MAP Kinase Kinase Kinase 5 Inhibitor, MAP3K5 Inhibitor, MAPKKK5 Inhibitor, MEKK5 Inhibitor, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-tert-butylbenzamide, 2HCl, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-(2-methyl-2-propanyl)benzamide, 2HCl, 4-tert-Butyl-N-(6-(1H-imidazol-1-yl)imidazo(1,2-a)pyridin-2-yl)benzamide, 2HCl
      DescriptionA cell-permeable imidazopyridine compound that acts as a potent, ATP-binding site-targeting ASK1/MEKK5-selective inhibitor (IC50 = 14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6), while exhibiting much reduced or no activity toward a panel of 195 other kinases, including MEKK1,TAK1, ERK1, JNK1, and p38α (IC50 >10 µM). Shown to inhibit STZ- (1 mM; Cat. No. 572201) induced JNK and p38 phosphorylation in INS-1 pancreatic β cells in a dose-dependent manner (IC50 <300 nM) and be orally available in rats in vivo (AUC0-8h = 275.4 ng·h/mL; 1 mg/kg p.o.).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1005775-56-3
      Chemical formulaC₂₁H₂₁N₅O • 2HCl
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (40 mg/ml)
      Storage -20°C
      Hygroscopic
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesTerao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.