JH530 is a potent methuosis inducer that suppresses the proliferation of triple-negative breast cancer (TNBC) cells by inducing complete intracellular vacuolization. It exhibits anti-tumor properties and is valuable for cancer research [1].

JH530 (Compound 5c) administered at concentrations of 1 μM or 2 μM for 24 hours induces significant morphological changes in HCC1806 cells characterized by intracellular vacuole accumulation but has minimal effects on the morphology and viability of 184B5 cells [1]. At doses of 0.5, 1.0, and 1.5 μM, JH530 prompts cell death through vacuolation after a 24-hour exposure [1]. Additionally, treatment with 1 μM JH530 effectively suppresses in vitro proliferation of TNBC cells [1], while a 1.5 μM concentration increases the expression of Rab7 and Lamp1 in HCC1806 and MDA-MB-468 cells [1]. Cell proliferation assays demonstrate significant anti-proliferative activity in vitro in HCC1806, MDA-MB-468, and HCC1937 TNBC cell lines, with IC50 values of 0.70 μM, 0.92 μM, and 1.03 μM respectively, after a 24-hour incubation at 1 μM [1]. Cell viability assays reveal distinct morphological changes at 1 μM in HCC1806 cells, marked by intracellular vacuoles, while effects on 184B5 cell morphology and viability are negligible [1]. Western Blot analysis shows a dose-dependent increase in Rab7 and Lamp1 expression, leading to cell death through vacuole formation [1]. Immunofluorescence studies confirm the induction of both Rab7 and Lamp1 in HCC1806 and MDA-MB-468 cells at 1.5 μM, resulting in substantial vacuole accumulation within most cells after 24 hours [1].

JH530 (compound 5c), administered via intraperitoneal injection at doses of 2.5 mg/kg or 5.0 mg/kg every two days for two weeks, significantly reduced tumor weight in the HCC1806 cell xenograft mouse model at 2.5 mg/kg and showed even more pronounced tumor suppression at 5 mg/kg [1].