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5.05420

Sigma-Aldrich

BMP Inhibitor III, LDN-212854

Synonym(s):

BMP Inhibitor III, LDN-212854, Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I

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About This Item

Empirical Formula (Hill Notation):
C25H22N6
Molecular Weight:
406.48
UNSPSC Code:
12352200
PubChem Substance ID:
60182388
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 25 mg/mL

storage temp.

2-8°C

SMILES string

C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3

General description

A 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).
A 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).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
ALK1/2/3
Reversible: yes
Secondary Target
RIP, Abl & PDGFR

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Preparation Note

Warming may be required for complete solubilization. Material will appear as a button in the bottom of the vial.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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