CJJ300

CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex[1].

Research Areas >> Cancer

IC50: 5.3 µM (TGF-β1-induced luciferase)[1]

CJJ300 disturbs protein-protein interactions and prevents TGF-β receptor dimerization (IC50 = 23.6 ± 5.8 µM)[1]. CJJ300 (0-80 µM, 2 h) inhibits the phosphorylation of intracellular mediators in the downstream TGF-β signaling pathways, and suppresses the expression of markers of EMT (epithelial-mesenchymal transition) without cytotoxicity[1]. CJJ300 suppresses TGF-β induced cell migration[1]. Western Blot Analysis[1] Cell Line: Human A549 lung epithelial cells Concentration: 20, 40, and 80 µM Incubation Time: 2 h Result: Significantly attenuated the increasement of P-Smad2/Smad3, P-Erk1/2 and P-Akt induced by TGF-β. Down regulated the expression of EMT-associated proteins, including fibronectin, α-SMA and MMP-2 in a dose-dependent manner.

[1]. Han Wu, et al. The development of a novel transforming growth factor-β (TGF-β) inhibitor that disrupts ligand-receptor interactions. Eur J Med Chem. 2020 Mar 1;189:112042.