505420 | BMP Inhibitor III, LDN-212854 - Calbiochem

505420
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₅H₂₂N₆

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05420.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable pyrazolopyrimidinylquinoline that is superior to Dorsomorphin (Cat. Nos. 171260 and 171261) and DMH1 (Cat. No. 203646) as an ATP-site-targeting, ALK1/2 inhibitor (IC50 = 2.40 and 1.30 nM, respectively; [ATP] = 6 µM) with respect to both potency and selectivity over ALK3/4/5 (IC50 = 0.858, 2.133, and 9.276 µM, respectively). Also a potent RIPK2 inhibitor (IC50 = 6 nM) with reduced potency against ABL1/c-abl, PDGFR-β, ALK3, and PDGFR-α (IC50 = 40, 68, 85.8, and 650 nM, respectively) and little inhibitory activity toward a panel of more than 190 kinases. Effectively inhibits ALK2- and ALK3-mediated C2C12 osteogenic differentiation (IC50 = 10 and 40.5 nM, respectively) in vitro and prevents constitutively active ALK2 Q207D mutant-induced heterotopic ossification in mice (6 mg/kg/12 h via i.p.) in vivo. A good complement to the ALK4/5/7-selective A-83-01 (Cat. No. 616454).
          Catalogue Number505420
          Brand Family Calbiochem®
          Synonyms5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I
          References
          ReferencesMohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
          Product Information
          FormPale yellow solid
          Hill FormulaC₂₅H₂₂N₆
          Chemical formulaC₂₅H₂₂N₆
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetALK1/2/3
          Secondary targetRIP, Abl & PDGFR
          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 Ambient Temperature Only
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Mohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.
          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.

          Revision17-January-2014 JSW
          Synonyms5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I
          DescriptionA cell-permeable pyrazolopyrimidinylquinoline that is superior to Dorsomorphin (Cat. Nos. 171260 and 171261) and DMH1 (Cat. No. 203646) as an ATP-site-targeting, ALK1/2 inhibitor (IC50 = 2.40 and 1.30 nM, respectively; [ATP] = 6 µM) with respect to both potency and selectivity over ALK3/4/5 (IC50 = 0.858, 2.133, and 9.276 µM, respectively). Also a potent RIPK2 inhibitor (IC50 = 6 nM) with reduced potency against ABL1/c-abl, PDGFR-β, ALK3, and PDGFR-α (IC50 = 40, 68, 85.8, and 650 nM, respectively), while displaying much reduced or no inhibitory activity toward a panel of more than 190 kinases. Selectively blocks BMP7-induced/ALK2-mediated SMAD1/5/8 activation in BMPR2-/- PASMC, but not TGF-β1-induced SMAD2 activation in PASMC. Effectively inhibits ALK2- and ALK3-mediated C2C12 osteogenic differentiation (IC50 = 10 and 40.5 nM upon stimulation with respective ligand BMP6 and BMP4) in vitro and prevents constitutively active ALK2 Q207D mutation-induced heterotopic ossification in mice (6 mg/kg/12 h via i.p.) in vivo. A good complement to the ALK4/5/7-selective A-83-01 (Cat. No. 616454).
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₅H₂₂N₆
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (25 mg/ml). Warming may be required for complete solubilization. Material will appear as a button in the bottom of the vial.
          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
          ReferencesMohedas, A.H., et al. 2013. ACS Chem. Biol. 8, 1291.