HJ-4

HJ-4 is a Piperine derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC) ^[1].

In Vivo, HJ-4 (8-32 μM, local application to tumor site, once daily for 7 days) inhibits angiogenesis in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids^[1].

In Vitro, HJ-4 (3.125-100 μM, 24 h) inhibits viability of CRC cells (HCT116: IC₅₀ = 15.82 μM; SW480: IC₅₀ = 20.46 μM)^[1]. HJ-4 (8-32 μM, 48 h) reduces colony number and size of HCT116/SW480 cells^[1]. HJ-4 (8-32 μM, 24 h) decreases EdU-positive HCT116/SW480 cells in EdU incorporation assay, dose-dependently inhibiting DNA synthesis^[1]. HJ-4 (8-32 μM, 0-48 h) inhibits adhesion, migration, and invasion of HCT116/SW480 cells^[1]. HJ-4 (8-32 μM, 24 h) upregulates p53, PUMA, BAX, cleaved caspase-3, cleaved PARP, and downregulates BCL-2, β-catenin, Cyclin D1 in HCT116/SW480 cells^[1]. HJ-4 (8-32 μM, 24 h) increases p53/BAX expression in HCT116/SW480 cells, and promotes YO-PRO-1 (early apoptosis) and PI (late apoptosis) positive cells in HCT116 cells via YO-PRO-1/PI staining^[1].

References:
[1]. Zhang L, et al. HJ-4, a novel piperine derivative, inhibits tumor growth and angiogenesis via p53 activation and oncogenic pathway inhibition in colorectal cancer models. Sci Rep. 2025 Sep 29;15(1):33541.