SJ6986
GSPT1 molecular glue / SJ6986 is a potent (IC50 = 15 nM for Cereblon; EC50 = 1.5 nM for MV4-11 AML cells), selective, and orally bioavailable molecular glue degrader of the small GTPases G1 to S phase transition 1/2 (GSPT1/2).1 It displayed selectivity for GPST1/2 over 9000 other proteins including the classic cereblon substrates IKZF1 (Ikaros) and IZKF3 (Aiolos). SJ6986 displayed efficacy against acute lymphoblastic leukemia cell lines and xenografts.2
Biochemicals & reagents
2765625-93-0
1 Nishiguchi et al. (2021), Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators; J. Med. Chem. 64 7296 2 Chang et al. (2023), The orally bioavailable GSPT1/2 degrader SJ6986 exhibits in vivo efficacy in acute lymphoblastic leukemia; Blood 142 629
-20°C
TARGET: Molecular glue; GTPase -- PATHWAY: Cell cycle; Degradation -- RESEARCH AREA: Ubiquitin/Proteasome -- DISEASE AREA: Cancer