HJC0152 (hydrochloride)

HJC0152 is an orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 µM, respectively, in MDA-MB-231 cells in a luciferase reporter assay).¹ It reduces total STAT3 and phosphorylated STAT3 levels in MDA-MB-231 cells and inhibits nuclear translocation of phosphorylated STAT3. HJC0152 inhibits proliferation of MCF-7 and MDA-MB-231 breast cancer and AsPC-1 and PANC-1 pancreatic cancer cells (IC₅₀s = 0.91, 1.64, 1.9, and 1.08 µM, respectively). It also halts the cell cycle at the G₀/G₁ phase, induces apoptosis, and suppresses cell proliferation in human head and neck squamous cell carcinoma cells.² HJC0152 (7.5 mg/kg, i.p. or 25 mg/kg, p.o.) inhibits tumor growth in an MDA-MB-231 breast cancer mouse xenograft model and in an orthotopic mouse model of squamous cell carcinoma.^1,2

WARNING This product is not for human or veterinary use.

1. Chen, H., Yang, Z., Ding, C., et al. Discovery of O-alkylamino tethered niclosamide derivatives as potent and orally bioavailable anticancer agents. ACS Med. Chem. Lett. 4(2), 180-185 (2013).

2. Wang, Y., Wang, S., Wu, Y., et al. Suppression of the growth and invasion of human head and neck squamous cell carcinomas via regulating STAT3 signaling and the miR-21/β-catenin axis with HJC0152. Mol. Cancer Ther. 16(4), 578-590 (2017).