PARP Agonist

ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC₅₀ = 0.113 μM, K_i = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers.

BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC₅₀ value of 0.28 μM and A_max ratio of 98%.

Stigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity.

ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.