LDN-193189

Normal development and tissue repair are controlled in part by SMADs, a family of intracellular proteins that are activated by signaling via serine/threonine kinase receptors of the TGF-beta superfamily. LDN-193189 inhibits SMAD1/5/8 phosphorylation by the bone morphogenetic protein (BMP) type I receptors, which are known as activin receptor-like kinases (ALKs), with an IC50 value of 4.9 nM. In in vitro kinase assays, it shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively). LDN-193189 has been used to inhibit BMP type I receptor activity to study the pathogenesis of fibrodysplasia ossificans progressive, a congenital hyperossification disorder, and to examine the role of osteogenesis in prostate tumor metastases in bone.Formal Name: 4-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. CAS Number: 1062368-24-4. Synonyms: DM-3189. Molecular Formula: C25H22N6. Formula Weight: 406.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: Chloroform: Slightly Soluble, DMSO: Slightly Soluble. lambdamax: 230, 332 nm. SMILES: N1(C2=CC=C(C(C=N3)=CN4C3=C(C5=CC=NC6=C5C=CC=C6)C=N4)C=C2)CCNCC1. InChi Code: InChI=1S/C25H22N6/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2. InChi Key: CDOVNWNANFFLFJ-UHFFFAOYSA-N.