DHRS11-IN-1 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 µM. DHRS11-IN-1 binds to DHRS11, forming a hydrogen bond with the enzymes His210 residue. DHRS11-IN-1 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. DHRS11-IN-1 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. DHRS11-IN-1 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. DHRS11-IN-1 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer[1].