A6Fdp4xds3

Rebecsinib is a splicing modulator and small molecule inhibitor of double-stranded RNA (dsRNA)-specific adenosine deaminase (adenosine deaminase acting on dsRNA; ADAR1), with potential immunomodulatory and antineoplastic activities. Upon intravenous administration, rebecsinib targets the splicing factor 3B (SF3B) core of the spliceosome at the interface of splicing factor 3B subunit 1 (SF3B1), 3 (SF3B3) and PHD finger-like domain-containing protein 5A (PHF5A) and inhibits the splicing of ADAR1 into the ADAR1p150 isoform, thereby inhibiting splicing-mediated ADAR1 activation. This inhibits ADAR1-mediated cancer stem cell (CSC) generation and CSC-mediated attenuation of the innate immune response, which may enhance antitumor immune responses and promote tumor cell killing. ADAR1, an enzyme that catalyzes the adenosine-inosine deamination of dsRNA, drives CSC generation and plays a key role in therapeutic resistance in many cancers.