HDAC-IN-30

HDAC-IN-30 is a novel multi-target HDAC inhibitor, including 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 exhibits potent antitumor efficacy[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

HDAC1:13.4 nM (IC50)

HDAC2:28.0 nM (IC50)

HDAC3:9.18 nM (IC50)

HDAC6:42.7 nM (IC50)

HDAC8:131 nM (IC50)

HDAC-IN-30 (compound 8 h; 0.5, 1, 2 μM; 48 hours) can effectively activate the p53 pathway by promoting the phosphorylation of p53[1].HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours; HepG2 cells) induces cell cycle arrest at the G2 phase in a concentration-dependent manner[1].HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours) possesses prominent anticancer activity in HepG2 cells[1]. Western Blot Analysis[1] Cell Line: HepG2 cells Concentration: 0.5, 1, 2 μM Incubation Time: 24 hours Result: Could effectively activate the p53 pathway by promoting the phosphorylation of p53 Cell Cycle Analysis[1] Cell Line: HepG2 cells Concentration: 0, 1, 2.5, 5 μM Incubation Time: 48 hours Result: Cells were arrested at the G2 phase in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: HepG2 cells Concentration: 0, 1, 2.5, 5 μM Incubation Time: 24 hours Result: Possessed prominent anticancer activity in HepG2 cells.

HDAC-IN-30 (12, 24 mg/kg; intraperitoneal injection, every two days for 4 weeks) exhibits potent anticancer activity and no side effects even at high dose (24 mg/kg)[1]. Animal Model: HepG2 xenograft mouse model[1] Dosage: 12, 24 mg/kg Administration: Intraperitoneal injection, every 2 days, 4 weeks Result: Exhibited potent anticancer activity

[1]. Liu Q, et al. Discovery of phthalazino [1, 2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. Eur J Med Chem. 2022, 229:114058.