LDN-212854

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair. LDN-212854 inhibits ALK2 (IC50 = 1.3 nM) in preference to other BMP type I receptors, ALK1 (IC50 = 2.4 nM) and ALK3 (IC50 = 85.8 nM) and with over 1,500-fold selectivity against the closely related activin and TGF-beta type I receptors (i.e., ALK4 and ALK5). It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC50 value of 10 nM. LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRbeta kinases with IC50 values less than 100 nM.Formal Name: 5-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. CAS Number: 1432597-26-6. Molecular Formula: C25H22N6. Formula Weight: 406.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml. lambdamax: 203, 241, 302 nm. SMILES: N1(C2=CC=C(C(C=N3)=CN4C3=C(C5=C(C=CC=N6)C6=CC=C5)C=N4)C=C2)CCNCC1. InChi Code: InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2. InChi Key: BBDGBGOVJPEFBT-UHFFFAOYSA-N.