Apoptosis inducer 7

Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Apoptosis inducer 7 (Compound 5I) (0.098-50 μM, 96 hours; human tumor cell lines) exerts the most potent antitumor activities against human cancer cell lines[1]. Apoptosis inducer 7 (Compound 5I) induces apoptosis in HCT-116 cells, and the apoptosis induction is related to the downregulation of anti-apoptotic protein c-Flip and upregulation of pro-apoptotic protein Noxa[1]. Cell Cytotoxicity Assay[1] Cell Line: Human breast cancer MDA-MB-231 cells, human lung cancer A549 cells, human colorectal cancer HCT-116 cells, human liver cancer HepG-2 cells and one non-tumor human breast epithelial MCF-10A cells. Concentration: 0.098-50 μM Incubation Time: 96 hours Result: Inhibited with IC50 values of 0.22, 0.15, 0.42, 0.14 and 1.03 μM for MDA-MB-231, A549, HCT-116, HepG-2 and MCF-10A, respectively. Cell Cycle Analysis[1] Cell Line: HCT-116 cells Concentration: 0.5, 0.75 and 1.0 μM Incubation Time: 24 hours Result: More than 40% of the cells were detected in the sub G1 phase. Western Blot Analysis[1] Cell Line: HCT-116 cells Concentration: 0.5, 0.75 and 1.0 μM Incubation Time: 24 hours Result: Induced cleavage of PARP, caspases and decreased the levels of c-Flip and HDAC3 proteins.

Apoptosis inducer 7 (Compound 5I) (5 mg/kg; i.p.; three times a week, for 14 days; LL/2 xenograft model in C57/ BL6J mice) inhibits tumor growth[1]. Animal Model: KARPAS-422 subcutaneous xenograft in mice[1] Dosage: 5 mg/kg Administration: Intraperitoneal injection; three times a week, for 14 days. Result: Inhibited the tumor growth with an inhibition rate of 62.3%, without significant body weight loss.

[1]. Huang M, et al. Synthesis and antitumor effects of novel 18β-glycyrrhetinic acid derivatives featuring an exocyclic α,β-unsaturated carbonyl moiety in ring A. Bioorg Chem. 2020 Oct;103:104187.