85-2071-74　BMP Inhibitor III, LDN-212854 (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) 5mg　217225

特徴

• A cell-permeable pyrazolopyrimidinylquinoline that is superior to Dorsomorphin and DMH1 as an ATP-site-targeting, ALK1/2 inhibitor (IC50 = 2.40 and 1.30nM, respectively; [ATP] = 6uM) with respect to both potency and selectivity over ALK3/4/5 (IC50 = 0.858, 2.133, and 9.276uM, respectively). Also a potent RIPK2 inhibitor (IC50 = 6nM) with reduced potency against ABL1/c-abl, PDGFR-beta, ALK3, and PDGFR-alpha (IC50 = 40, 68, 85.8, and 650nM, 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 40.5nM, respectively) in vitro and prevents constitutively active ALK2 Q207D mutant-induced heterotopic ossification in mice (6mg/kg/12h via i.p.) in vivo.
• Synonyms: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
• Primary Target:ALK1/2/3
• Secondary Target:RIP, Abl & PDGFR
• Solubility:DMSO
• Molecular Formula:C₂₅H₂₂N₆
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.