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505420 BMP Inhibitor III, LDN-212854 - Calbiochem

BMP Inhibitor III, LDN-212854 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

Primary Target: ALK1/2/3
505420
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₅H₂₂N₆

Products

Catalogue NumberPackaging Qty/Pack
5.05420.0001 Glass bottle 5 mg
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®
SynonymsAbl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
5.05420.0001 04055977243840

Documentation

BMP Inhibitor III, LDN-212854 - Calbiochem 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
SynonymsAbl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
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 Protect from light
+2°C to +8°C
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.