SAG 21k

SAG 21k is an agonist of the hedgehog signaling pathway. It activates the Smoothened receptor (Smo) in a reporter assay using C3H/10T1/2 cells expressing Smo (EC50 = 0.3 nM). SAG 21k (1 nM) increases the levels of mRNA encoding Ki67, coiled-coil domain-containing protein 1 (Ccdc1), collagen II, alkaline phosphatase (ALP), nuclear glioma-associated oncogene 1 (Gli1), and Gli2, and decreases the levels of mRNA encoding matrix metalloproteinase-13 (MMP-13) in mouse primary chondrocytes. In vivo, SAG 21k (5 mg/kg per day), in combination with the PHD2 antagonist IOX2 (Cay-11573), induces the formation of bone calluses and partial bone unions and increases total bone volume, but not total tissue volume, in a mouse model of surgery-induced non-healing bone fracture.Formal Name: 3-chloro-4,7-difluoro-N-[[2-methoxy-5-(4-pyridinyl)phenyl]methyl]-N-[trans-4-(methylamino)cyclohexyl]-benzo[b]thiophene-2-carboxamide. CAS Number: 946002-48-8. Molecular Formula: C29H28ClF2N3O2S. Formula Weight: 556.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly soluble: 0.1-1 mg/ml, Ethanol: Sparingly soluble: 1-10 mg/ml. SMILES: ClC(C1=C(F)C=C2)=C(C(N([C@H]3CC[C@@H](CC3)NC)CC4=C(OC)C=CC(C5=CC=NC=C5)=C4)=O)SC1=C2F. InChi Code: InChI=1S/C29H28ClF2N3O2S/c1-33-20-4-6-21(7-5-20)35(29(36)28-26(30)25-22(31)8-9-23(32)27(25)38-28)16-19-15-18(3-10-24(19)37-2)17-11-13-34-14-12-17/h3,8-15,20-21,33H,4-7,16H2,1-2H3/t20-,21-. InChi Key: YVIFQUJDZSAFKG-MEMLXQNLSA-N.