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GSPT1 degrader-17

GSPT1 degrader-17 (Compound 9q) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1) . GSPT1 degrader-17 degrades GSPT1 in U937 cells with a DC50 of 35 nM and Dmax of 81.65%. GSPT1 degrader-17 has a strong inhibitory effect on U937, MOLT-4 and MV4-11 cells with IC50 values of 0.019, 0.006 and 0.027 μM. GSPT1 degrader-17 can induce cells apoptosis and G0/G1 phase arrest. GSPT1 degrader-17 can be used for the research of cancer, such as acute myeloid leukemia[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Molecular Glues

Related Pathways

Apoptosis; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C1C2=CC(CCC(NC3=CC(N(CCOC)C)=C(C)C(Cl)=C3)=O)=CC=C2CN1C4C(NC(CC4)=O)=O

Molecular Formula

C27H31ClN4O5

Molecular Weight

527.01

References & Citations

[1]Wei Y, et al. Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders. Eur J Med Chem. 2023 Oct 5;258:115580.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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