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Field of application
D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
LC-04-045 is a leading NEK7 molecular glue degrader with DC50 of 7 nM and Dmax of 90 % in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome.
PVTX-405 is a potent, effective, highly selective, and orally efficacious IKZF2 molecular glue degrader with DC50 of 0.7 nM. PVTX-405 in combination with anti-PD1 or anti-LAG3 significantly increases animal survival compared to anti-PD1 or anti-LAG3 alone.
MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.