GSPT1 degrader-17

GSPT1 degrader-17 (compound 9q) (3.7-300 nM; 2-24 h) potently induces dose- and time-dependent degradation of GSPT1 in U937 cells, with a DC₅₀ of 35 nM, and reduces the biological half-life of GSPT1 to 6.3 h^[1].
GSPT1 degrader-17 (3.7-300 nM; 6 h) potently induces dose-dependent degradation of GSPT1 in MOLT-4 and MV4-11 leukemia cells^[1].
GSPT1 degrader-17 (100 nM; 6 h, with 2 h pre-treatment) induces the degradation of GSPT1 in U937 cells via the ubiquitin-proteasome system, which is evidenced by the experimental results that proteasome/NAE inhibitors restore GSPT1 levels and the ubiquitination level of GSPT1 is elevated ^[1].
GSPT1 degrader-17 (3.7-300 nM; 6 h) is a highly selective GSPT1 degrader in U937 cells, which induces a significant reduction in GSPT1, while no degradation of the CRBN neosubstrates IKZF1, IKZF3 or CK1α is detected^[1].
GSPT1 degrader-17 (72 h) potently inhibits the proliferation of U937, MOLT-4, and MV4-11 leukemia cells, with IC₅₀ values ranging from 0.006 to 0.027 μM^[1].

GSPT1 degrader-17 (10-100 nM; 24 h) induces G0/G1 phase arrest and apoptosis in U937 cells in a dose-dependent manner after 24 h of treatment, accompanied by decreased expression of cell cycle regulatory proteins and increased expression of apoptotic markers^[1].