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

509882
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Empirical FormulaCAS #
C₂₅H₂₂N₆ • 4HCl•3H₂O 1062368-62-0

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      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®
      SynonymsBone Morphogenetic Protein Inhibitor IV, RIPK2 Inhibitor II, DM-3189, ALK2/3/6 Inhibitor, LDN193189, RIP2 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
      Quality LevelMQ100
      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

      BMP Inhibitor IV, LDN-193189 - CAS 1062368-62-0 - Calbiochem 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
      SynonymsBone Morphogenetic Protein Inhibitor IV, RIPK2 Inhibitor II, DM-3189, ALK2/3/6 Inhibitor, LDN193189, RIP2 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.