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171260 AMPK Inhibitor, Compound C - CAS 866405-64-3 - Calbiochem

171260
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₄H₂₅N₅O866405-64-3

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171260-10MGCN
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      Plastic ampoule 10 mg
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      171260-5MGCN
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          Description
          OverviewA cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50 = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100 = 2.5 µM) and VEGF signaling-dependent intersomitic vessel formation (EC50 = 5 µM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No. 123040) and/or Metformin (Cat. No. 317240) for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. Also available as a 10 mM solution in DMSO (Cat. No. 171261).
          Catalogue Number171260
          Brand Family Calbiochem®
          Synonyms6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine, Dorsomorphin, AMPK Inhibitor I, BMP Inhibitor I
          References
          ReferencesHao, J., et al. 2010. ACS Chem.Biol. 5, 245.
          Yu, P.B., et al. 2008. Nat. Chem. Biol 4, 33.
          Kim, E.K., et al. 2004. J. Biol. Chem. 279, 19970.
          Lee, M., et al. 2003. J. Biol. Chem. 278, 39653.
          Inoki, K., et al. 2003. Cell 115, 577.
          Fryer, L.G., 2002. FEBS Lett. 531, 189.
          Zhou, G., et al. 2001. J. Clin. Invest. 108, 1167.
          Product Information
          CAS number866405-64-3
          ATP CompetitiveY
          FormLight yellow solid
          Hill FormulaC₂₄H₂₅N₅O
          Chemical formulaC₂₄H₂₅N₅O
          ReversibleY
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetAMPK
          Primary Target IC<sub>50</sub>25.1, 148, and 234.6 nM, against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity, respectively
          Primary Target K<sub>i</sub>EC100 = 2.5 µM against BMP pathway-dependent dorsoventral development; EC50 = 5 µM against VEGF signaling-dependent intersomitic vessel formation in zebrafish embryo in vivo
          Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          AMPK Inhibitor, Compound C - CAS 866405-64-3 - Calbiochem Certificates of Analysis

          TitleLot Number
          171260

          References

          Reference overview
          Hao, J., et al. 2010. ACS Chem.Biol. 5, 245.
          Yu, P.B., et al. 2008. Nat. Chem. Biol 4, 33.
          Kim, E.K., et al. 2004. J. Biol. Chem. 279, 19970.
          Lee, M., et al. 2003. J. Biol. Chem. 278, 39653.
          Inoki, K., et al. 2003. Cell 115, 577.
          Fryer, L.G., 2002. FEBS Lett. 531, 189.
          Zhou, G., et al. 2001. J. Clin. Invest. 108, 1167.
          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.

          Revision22-March-2012 JSW
          Synonyms6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine, Dorsomorphin, AMPK Inhibitor I, BMP Inhibitor I
          DescriptionA cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50 = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100 = 2.5 µM) and VEGF signaling-dependent intersomitic vessel formation (EC50 = 5 µM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No. 123040) and/or Metformin (Cat. No. 317240) for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. Also available as a 10 mM solution in DMSO (Cat. No. 171261).
          FormLight yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number866405-64-3
          Chemical formulaC₂₄H₂₅N₅O
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (4 mg/ml), 2% HCl (10 mg/ml), 2% Acetic Acid (10 mg/ml), or Methanol (3 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesHao, J., et al. 2010. ACS Chem.Biol. 5, 245.
          Yu, P.B., et al. 2008. Nat. Chem. Biol 4, 33.
          Kim, E.K., et al. 2004. J. Biol. Chem. 279, 19970.
          Lee, M., et al. 2003. J. Biol. Chem. 278, 39653.
          Inoki, K., et al. 2003. Cell 115, 577.
          Fryer, L.G., 2002. FEBS Lett. 531, 189.
          Zhou, G., et al. 2001. J. Clin. Invest. 108, 1167.