PYZD 4409

  • Chemical Properties
CAS No. 423148-78-1 Cat. No. BCP29044
Name PYZD 4409
Synonyms PYZD-4409;PYZD4409;
Formula C14H7ClFN3O5 M. Wt 351.67
  • Biological Activity
Description PYZD-4409 is an inhibitor of ubiquitin-activating enzyme UBA1 (E1). PYZD-4409 induced cell death in malignant cells and preferentially inhibited the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells. Mechanistically, genetic or chemical inhibition of E1 increased expression of E1 stress markers. Moreover, BI-1 overexpression blocked cell death after E1 inhibition, suggesting ER stress is functionally important for cell death after E1 inhibition. Finally, in a mouse model of leukemia, intraperitoneal administration of PYZD - 4409 decreased tumor weight and volume compared with control without untoward toxicity.
Pathways Protease/Metabolic Enzyme 
Targets E1 E2 E3 Enzyme 

Structure

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