| Bioactivity | J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC50 of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis[1]. |
| Invitro | J-1063 (compound 4) (10 mM) shows significant ALK5 inhibitory activity (IC50s of 8.12 and 0.039 µM for p38α MAP kinase and ALK5, respectively)[1].J-1063 (2.5, 5, 10 µM; 1 h) improved fibroblast differentiation induced by TGF-β in LX-2 cells[1].J-1063 (2.5, 5, 10 µM; 1 h) inhibits the inflammatory response induced by TGF-β[1].J-1063 inhibits liver fibrosis by regulating TGF-β/Smad signaling and inhibits the activation of NLPR3-Caspase-1 inflammasome[1].J-1063 (12.5 mg/kg; Cxcl1, Cxcl2 cells) inhibits the infiltration of macrophages and neutrophils during liver fibrosis[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | J-1063 (12.5, 25, 50 mg/kg; i.g., one time per day for two weeks) shows no toxic side effects on mice at low dose and is suitable for therapeutic administration[1].J-1063 (12.5 mg/kg; p.o., daily for two consecutive weeks) shows benefit for TAA-induced liver fibrosis in mice[1]. Animal Model: |
| Name | J-1063 |
| CAS | 2374772-46-8 |
| Formula | C24H19N5OS |
| Molar Mass | 425.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zheng GH, et al. The in vitro and in vivo study of a pyrazole derivative, J-1063, as a novel anti-liver fibrosis agent: Synthesis, biological evaluation, and mechanistic analysis. Bioorg Chem. 2022; 122:105715. |