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

178506
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      Overview

      Replacement Information

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      178506-10MG
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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
          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

          Reference overview
          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.