218696 | Casein Kinase I Inhibitor, D4476 - CAS 301836-43-1 - Calbiochem

218696
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      Overview

      Key Spec Table

      Empirical Formula CAS #
      C₂₃H₁₈N₄O₃301836-43-1

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      218696-1MG
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          1 mg
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          Description
          Overview A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 µM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 0.5 µM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and only weakly affects the activities of a panel of kinases tested, including PKB, SGK and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1a in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
          Catalogue Number 218696
          Brand Family Calbiochem®
          Synonyms CK1 Inhibitor, 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide
          References
          References Rena, G., et al. 2004. EMBO Reports 5, 60.
          Product Information
          CAS number 301836-43-1
          ATP Competitive Y
          Form Crystalline solid
          Hill Formula C₂₃H₁₈N₄O₃
          Chemical formula C₂₃H₁₈N₄O₃
          Molar Mass 398.4
          Reversible Y
          Structure formula Image
          Applications
          Biological Information
          Primary Target CK1, CK1d
          Primary Target IC50 0.2 µM against CK1 from S. pombe; 0.3 µM for CK1δ 0.5 µM against ALK5
          Purity ≥95% by HPLC
          Physicochemical Information
          Cell permeable Y
          Solubility DMSO
          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 +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze No
          Special Instructions Following 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

          MSDS

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          Certificates of Analysis

          TitleLot Number
          218696

          References

          Reference overview
          Rena, G., et al. 2004. EMBO Reports 5, 60.
          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.

          Revision 30-November-2009 RFH
          Synonyms CK1 Inhibitor, 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl)benzamide
          Description A cell-permeable, reversible, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 200 nM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 500 nM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~ 10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
          Form Crystalline solid
          Intert gas (Yes/No) Packaged under inert gas
          Recommended reaction conditions For use in cell culture medium dilute 1 µl of 40 mg/ml stock solution in a mixture of 6 µl serum-free medium and 3 µl GeneJuice® Transfection Reagent (Cat. No. 70967) at +21°C; add the mixture dropwise with swirling to cultured cells.
          CAS number 301836-43-1
          Molar mass 398.4
          Chemical formula C₂₃H₁₈N₄O₃
          Structure formula
          Purity ≥95% by HPLC
          Solubility DMSO (40 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          References Rena, G., et al. 2004. EMBO Reports 5, 60.