TP-008

TP-008 is an inhibitor of activin receptor-like kinase 4 (ALK4) and ALK5, also known as TGF-beta receptor type 1 (TGF-betaRI, IC50s = 113 and 343 nM, respectively). It is selective for ALK4 and ALK5 over a panel of 467 kinases at 1 µM. TP-008 inhibits ALK4 or ALK5 signaling in a reporter assay using HEK293 cells expressing ALK4 or ALK5 (IC50s = 526 and 245 nM, respectively). It inhibits TGF-beta1-induced increases in the levels of phosphorylated Smad2 in C2C12 mouse skeletal muscle myoblasts when used at concentrations of 1 or 10 µM. In vivo, TP-008 (150 or 500 mg/kg per day) induces valvular interstitial cell proliferation, neutrophil infiltration, hemorrhage, and fibrin deposition in rat heart valves.Formal Name: 1-[2-(5-chloro-2-fluorophenyl)-5-methyl-4-pyridinyl]-1,2-dihydro-2-oxo-3H-imidazo[4,5-c]pyridine-3-acetamide. CAS Number: 1976038-41-1. Molecular Formula: C20H15ClFN5O2. Formula Weight: 411.8. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C1N(C(C=C(C(C=C2Cl)=C(C=C2)F)N=C3)=C3C)C4=CC=NC=C4N1CC(N)=O. InChi Code: InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28). InChi Key: LVEUPFUJRKZPEN-UHFFFAOYSA-N.