MilliporeSigma™ Calbiochem™ BMP Inhibitor III, LDN-212854

Description

A cell-permeable pyrazolopyrimidinylquinoline that is superior to Dorsomorphin (Cat

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] = 6μM) with respect to both potency and selectivity over ALK3/4/5 (IC₅₀ = 0.858, 2.133, and 9.276μM, respectively). Also a potent RIPK2 inhibitor (IC₅₀ = 6nM) 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 (6mg/kg/12 h via i.p.) in vivo. A good complement to the ALK4/5/7-selective A-83-01 (Cat. No. 616454).

Specifications

• Color: Pale Yellow
• Description: 98% by HPLC
• Target Proteins: ALK1/2/3
• Molecular Formula: C₂₅H₂₂N₆
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 5 mg