509882 | BMP Inhibitor IV, LDN-193189 - CAS 1062368-62-0 - Calbiochem

509882
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₂₂N₆ • 4HCl•3H₂O 1062368-62-0

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      5.09882.0001
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          Glass bottle 10 mg
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          Description
          Overview

          This product has been discontinued.



          A cell-permeable pyrazoloquinoline analog of Dorsomorphin (AMPK Inhibitor, Compound C, Cat. No. 480066) that potently inhibits the transcriptional activity of BMP type 1 receptors ALK 2 and 3 (IC50 = 5 and 30 nM, respectively) with minimal effect on activin and the TGF-β type 1 receptors ALK4, 5, and 7 (IC50 ~500 nM). Also reported to block the activity of RIPK2 (IC50 = 25 nM) and germinal central kinase (GCK; IC50 = 80 nM). At higher concentration, it inhibits the activity of ALK6 (IC50 = 150 nM). Also reported to block BMP-4- induced phosphorylation of SMAD 1, 5, and 8 (IC50 ~ 5 nM) in murine pulmonary artery smooth muscle cells. Shown to be about 200-fold more potent when compared to Dorsomorphin. Exhibits desirable pharmacokinetic properties with a half life of 1.6 h, low clearance in liver microsomes (CLint = 16.9 ml/min/mg protein), and a satisfactory exposure following a single intraperitoneal dose of 3 mg/kg in mice (AUC = 1000 ng . h/ml). Directs differentiation of pluripotent stem cells toward a specified lineage.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.

          Catalogue Number509882
          Brand Family Calbiochem®
          SynonymsDM-3189, ALK2/3/6 Inhibitor, LDN193189, RIP2 Inhibitor II, Bone Morphogenetic Protein Inhibitor IV, RIPK2 Inhibitor II
          References
          ReferencesMohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
          Chambers, S.M., et al. 2012. Nat. Biotechnol. 30, 715.
          Vogt, J., et al. 2011. Cell. Signal. 23, 1831.
          Hao, J., et al. 2010. ACS Chem. Biol. 5, 245.
          Cuny, G.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 4388.
          Yu, P.B., et al. 2008. Nat. Med. 14, 1363.
          Product Information
          CAS number1062368-62-0
          FormYellow liquid
          FormulationSupplied as a 10 mM solution (10 mg in 1.65 ml) in H₂O.
          Hill FormulaC₂₅H₂₂N₆ • 4HCl•3H₂O
          Chemical formulaC₂₅H₂₂N₆ • 4HCl•3H₂O
          ReversibleY
          Applications
          Biological Information
          Primary TargetALK2/3/6
          Secondary targetRIPK2, GCK
          Purity≥98% 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 Dry Ice Only
          Toxicity Standard Handling
          Storage ≤ -70°C
          Do not freeze Ok to freeze
          Special InstructionsFollowing initial thaw, 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Mohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
          Chambers, S.M., et al. 2012. Nat. Biotechnol. 30, 715.
          Vogt, J., et al. 2011. Cell. Signal. 23, 1831.
          Hao, J., et al. 2010. ACS Chem. Biol. 5, 245.
          Cuny, G.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 4388.
          Yu, P.B., et al. 2008. Nat. Med. 14, 1363.
          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.

          Revision02-May-2014 JSW
          SynonymsDM-3189, ALK2/3/6 Inhibitor, LDN193189, RIP2 Inhibitor II, Bone Morphogenetic Protein Inhibitor IV, RIPK2 Inhibitor II
          DescriptionA cell-permeable pyrazoloquinoline analog of Dorsomorphin (AMPK Inhibitor, Compound C, Cat. No. 480066) that potently inhibits the transcriptional activity of BMP type 1 receptors ALK 2 and 3 (IC50 = 5 and 30 nM, respectively) with minimal effect on activin and the TGF-β type 1 receptors ALK4, 5, and 7 (IC50 ~500 nM). Also reported to block the activity of RIPK2 (IC50 = 25 nM) and germinal central kinase (GCK; IC50 = 80 nM). At higher concentration, it inhibits the activity of ALK6 (IC50 = 150 nM). Also reported to block BMP-4- induced phosphorylation of SMAD 1, 5, and 8 (IC50 ~ 5 nM) in murine pulmonary artery smooth muscle cells. Shown to be about 200-fold more potent when compared to Dorsomorphin. Exhibits desirable pharmacokinetic properties with a half life of 1.6 h, low clearance in liver microsomes (CLint = 16.9 ml/min/mg protein), and a satisfactory exposure following a single intraperitoneal dose of 3 mg/kg in mice (AUC = 1000 ng . h/ml). Directs differentiation of pluripotent stem cells toward a specified lineage.
          FormYellow liquid
          FormulationSupplied as a 10 mM solution (10 mg in 1.65 ml) in H₂O.
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1062368-62-0
          Chemical formulaC₂₅H₂₂N₆ • 4HCl•3H₂O
          Purity≥98% by HPLC
          SolubilityH₂O (10 mg/ml)
          Storage ≤ -70°C
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesMohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
          Chambers, S.M., et al. 2012. Nat. Biotechnol. 30, 715.
          Vogt, J., et al. 2011. Cell. Signal. 23, 1831.
          Hao, J., et al. 2010. ACS Chem. Biol. 5, 245.
          Cuny, G.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 4388.
          Yu, P.B., et al. 2008. Nat. Med. 14, 1363.