PARP1 Activator

Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease.

Prostaglandin A2 (PGA2) is a Cyclopentenone prostaglandin. Prostaglandin A2 induces Caspase-dependent Apoptosis, activates p53. Prostaglandin A2 activates ERK2 and JNK1/SAPK. Prostaglandin A2 shows antiviral activity against HSV-1. Prostaglandin A2 has anti-tumor effects. Prostaglandin A2 can be used for the research of colorectal cancer, colorectal carcinoma, breast carcinoma, and herpetic keratitis.

Bcl-2/Mcl-1-IN-5 (Compound S6) is a Bcl-2 and Mcl-1 inhibitor. Bcl-2/Mcl-1-IN-5 promotes Apoptosis, downregulates anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane potential depolarization, and activates the Caspase-dependent apoptotic cascade, as evidenced by Caspase-3 activation and PARP1 cleavage. Bcl-2/Mcl-1-IN-5 has anti-hepatocellular carcinoma activity.

HL435 is a BRD4 PROTAC degrader with DC₅₀ values of 11.9 nM (MDA-MB-231 cells) and 21.9 nM (MCF-7 cells), respectively. HL435 recruits the CRL4_DCAF11 E3 ubiquitin ligase complex to degrade BRD4 via the ubiquitin-proteasome system. HL435 induces cell cycle arrest and apoptosis (apoptosis) in cancer cells, downregulates the expression levels of cyclin D1 and cyclin B1, activates caspase-9, and induces PARP1 cleavage. HL435 exerts anti-tumor activity both in vitro and in mouse xenograft tumor models. HL435 can be used for the research of breast cancer and prostate cancer.

CM002 is a circadian clock activator. CM002 inhibits the lineage commitment and terminal differentiation of preadipocytes by activating the circadian clock, thereby blocking the adipogenesis process driven by Wnt signaling-mediated transcriptional induction. CM002 attenuates lipid storage in a clock-dependent manner via inhibition of the lipogenic program in mature adipocytes. CM002 enhances circadian clock output across various adipose depots in both lean and obese mice through BMAL1/CLOCK-dependent metabolic reprogramming, inhibits adipocyte development and hypertrophy, and improves insulin sensitivity. CM002 can be used in research on obesity and type 2 diabetes.

TPP-C8-CO-DSG bromide is a derivative of Diosgenin (HY-N0177) and an anticancer agent. TPP-C8-CO-DSG bromide downregulates Bcl-2 expression and upregulates Bax expression. TPP-C8-CO-DSG bromide promotes the cleavage of Caspase 9, Caspase 3 and PARP-1. TPP-C8-CO-DSG bromide depolarizes mitochondrial membrane potential, reduces intracellular ATP production, and induces intracellular ROS accumulation. TPP-C8-CO-DSG bromide promotes Apoptosis. TPP-C8-CO-DSG bromide exhibits anticancer activity against prostate cancer, breast cancer, lung adenocarcinoma, cervical cancer and colorectal cancer. TPP-C8-CO-DSG bromide can be used in the research of cervical cancer.

IDO1-IN-34 is a selective IDO1 inhibitor with an IC₅₀ of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia.

Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer.

DZ-1-DHA is a conjugate of DHA (HY-B2167) and DZ-1 dye. DZ-1-DHA mediates selective cellular uptake via binding to overexpressed OATP1A2. DZ-1-DHA induces the cleavage of Caspase-3, Caspase-8, Caspase-9 and PARP-1. DZ-1-DHA induces Apoptosis and Ferroptosis. DZ-1-DHA induces ROS production through a Fenton-like mechanism, causes mitochondrial membrane depolarization, and triggers lipid peroxidation. DZ-1-DHA can be used in studies related to colorectal cancer liver metastasis.