YH-306

YH-306 is an anticancer agent.¹ It reduces TGF-β-induced transcriptional activity by 72.4% in a reporter assay using HaCaT cells when used at a concentration of 1 µM. YH-306 inhibits the proliferation of PC-9, H1299, and A549 lung cancer cells (IC₅₀s = 5.87, 8.07, and 7.9 µM, respectively). It decreases migration of H1299 cells in a wound healing assay when used at concentrations of 0.1, 0.5, or 1 µM. YH-306 (50 µM) inhibits actin polymerization in HT-29 colon cancer cells.² It inhibits fibronectin-induced increases in the levels of matrix metalloproteinase-2 (MMP-2), MMP-9, and phosphorylated focal adhesion kinase (FAK), PI3K, and ERK in CT26 colon cancer cells when used at a concentration of 50 µM. YH-306 (5 mg/kg per day) decreases tumor volume without reducing body weight in an A549 mouse xenograft model.¹ It also reduces tumor growth and the number of hepatic metastases in a CT26-luc colon cancer mouse xenograft model with hepatic metastases when administered at a dose of 50 mg/kg per day.²

WARNING This product is not for human or veterinary use.

1. Zheng, C., Fang, Y., Tong, W., et al. Synthesis and biological evaluation of novel tetrahydro-β-carboline derivatives as antitumor growth and metastasis agents through inhibiting the transforming growth factor-β signaling pathway. J. Med. Chem. 57(3), 600-612 (2014).

2. Dai, F., Chen, Y., Huang, L., et al. A novel synthetic small molecule YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. J. Cell. Mol. Med. 19(2), 383-395 (2015).