HDAC-IN-30 is a multi-target HDAC inhibitor. HDAC-IN-30 inhibits HDAC1 (IC50 =13.4 nM), HDAC2 (IC50 =28.0 nM), HDAC3 (IC50 =9.18 nM), HDAC6 (IC50 =42.7 nM), HDAC8 (IC50 =131 nM). HDAC-IN-30 shows potent antitumor efficacy.

HDAC2:28.0 nM, HDAC3:9.18 nM, HDAC6:42.7 nM, HDAC8:131 nM, HDAC1:13.4 nM

HDAC-IN-30, referred to as compound 8 h at concentrations of 0.5, 1, and 2 μM for 48 hours, effectively activates the p53 pathway through enhanced phosphorylation of p53. At increased dosages (0, 1, 2.5, 5 mM; 48 hours) in HepG2 cells, it leads to a concentration-dependent cell cycle arrest at the G2 phase, demonstrating significant anticancer activity. Western Blot analysis confirms its role in p53 pathway activation by promoting p53 phosphorylation, whereas cell cycle and apoptosis analyses reveal its capability to induce G2 phase arrest and pronounce anticancer effects in HepG2 cells over a 48-hour period.

HDAC-IN-30, administered via intraperitoneal injection at doses of 12 and 24 mg/kg every two days over a period of four weeks, demonstrated significant anticancer efficacy without adverse effects, even at the higher dosage of 24 mg/kg, in the HepG2 xenograft mouse model [1].