Stenoparib

Stenoparib (CAS No.: 1140964-99-3) is a synthetic small molecule for biomedical research and drug discovery development, classified as a dual-target inhibitor that simultaneously inhibits poly(ADP-ribose) polymerase 1/2 (PARP1/2) and tankyrase 1/2 (TNKS1/2). It interferes with poly(ADP-ribosyl)ation-dependent single-strand DNA break repair and chromatin-associated DNA damage responses by inhibiting PARP catalytic activity, while also inhibiting tankyrase to stabilize AXIN and reduce the output of the Wnt/β-catenin signaling pathway, thereby supporting analysis of pathway crosstalk and functional linkage related to tumor biology. In in vitro studies, it shows inhibitory activity against PARP1/2 in the low nanomolar range and against TNKS1/2 at tens of nanomolar levels, while its effects on other PARP family members are generally reduced to the micromolar range; in cellular models, it can bind chromatin in a concentration-dependent manner, inhibit cell proliferation in PARP-dependent contexts, and reduce the expression of effector molecules such as AXIN2, total and active β-catenin, and Cyclin D1. Typical research applications include target validation, synthetic lethality mapping in homologous recombination-deficient systems, reversible modulation of the Wnt signaling pathway, and combination screening with DNA damage-inducing factors; in animal models, it is also used to evaluate pathway engagement, changes in molecular biomarkers, and quantification of growth-related phenotypes, with the concentrations or doses used in experiments generally depending on the specific experimental design and research objectives. Also known as E7449, 2X?121, and MGI25036, this product is for research use only and is not intended for human or veterinary use, diagnosis, food, cosmetics, or any form of clinical application.