Caspase 7 Inducer

SK2188 (JB325) is a highly efficient and selective PROTAC degrader targeting AURKA (DC₅₀ = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma.

Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.

PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC₅₀ values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC).

Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC₅₀ = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells.

Clerodin (3-Deoxycaryoptinol) is a natural diterpenoid compound that can be isolated from traditional Chinese medicinal plants such as Clerodendrum infortunatum. Clerodin exhibits caspase-3 regulation, apoptosis induction, cell cycle arrest, ROS induction and glutathione depletion effects, along with anti-cancer and antifeedant activities. It shows selective cytotoxicity against leukemia cells and breast cancer cells, but has no obvious toxicity to normal human blood cells and lymphocytes. Clerodin also reduces the feeding behavior of Helicoverpa armigera larvae on cabbage leaf discs, but has no significant contact toxicity to these larvae. Clerodin can be used in research related to acute monocytic leukemia and human breast cancer.