GSPT1 degrader-2

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

PROTACGSPT1 degrader-2 (compound A) acts as a molecular glue for GSPT1, achieving degradation efficiencies exceeding 95%. Meanwhile, GSPT1 degrader-8 exhibits inhibitory effects on HL-60 cells, demonstrating an IC50 of 10 nM.

SJ6986 is a potent, selective, and orally active GSPT1 2 degrader, effectively degrading GSPT1 with a DC50 of 2.1 nM (D max 99%) [1].

C-Myc Inhibitor 7, serving as both a c-Myc inhibitor and a multi-target protein degrader, effectively degrades proteins c-MYC, CK1α, GSPT1, and IKZF1 2 3 across various tumor cell types. It holds potential for research into diseases associated with high c-Myc expression, including cancer, cardiovascular and cerebrovascular conditions, and viral infections.

Thalidomide 5-Pip-C-oxotetrahydropyrimidin-bromophenyl, an E3 Ligase Ligand-Linker Conjugate, serves as a precursor for synthesizing PROTAC GSPT1 degrader-2.

PROTACerf3a Degrader-2 (Compound C59) is an orally active degrader of PROTACerf3a that suppresses the expression levels of SRD5A3 and GSPT1 (eRF3a). It inhibits the proliferation of cancer cells, such as in 22Rv1. PROTACerf3a Degrader-2 is utilized in research for various cancers including prostate, ovarian, liver, cervical, leukemia, and breast cancer.