RBN012759

RBN012759 is a potent, selective, and orally active small molecule inhibitor of Poly(ADP-Ribose) Polymerase 14 (PARP14), developed by Ribon Therapeutics. It exhibits high potency with a biochemical IC50 of less than 3 nM and demonstrates significant selectivity (greater than 300-fold) over other PARP family members. RBN012759 functions by inhibiting PARP14-specific self-MARylation, which in turn reverses IL-4-driven pro-tumor gene expression in macrophages. This mechanism is designed to reprogram the tumor microenvironment from an immunosuppressive state to an inflammatory, anti-tumor state. The compound is being investigated for its potential to sensitize tumors, such as muscle-invasive bladder cancer, to chemotherapy and is also being explored for applications in acute myeloid leukemia (AML) and allergic inflammatory conditions like asthma.

Other names

CAS 2360851-29-0CAS2360851-29-0CAS-2360851-29-0