A-77-01

A-77-01 is a potent inhibitor of the TGF-beta1 receptor ALK5 (IC50 = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-beta on lung epithelial Mv1Lu cells. It completely blocks phosphorylation of SMAD2 by TGF-beta in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-beta.Formal Name: 4-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-quinoline. CAS Number: 607737-87-1. Molecular Formula: C18H14N4. Formula Weight: 286.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 14 mg/ml, DMSO:PBS (pH 7.2) (1:20): 0.04 mg/ml, Ethanol: 1 mg/ml. lambdamax: 229, 286 nm. SMILES: CC1=NC(C2=NNC=C2C3=CC=NC4=C3C=CC=C4)=CC=C1. InChi Code: InChI=1S/C18H14N4/c1-12-5-4-8-17(21-12)18-15(11-20-22-18)13-9-10-19-16-7-3-2-6-14(13)16/h2-11H,1H3,(H,20,22). InChi Key: KJTYZDORHCDZPS-UHFFFAOYSA-N.