PYZD-4409

PYZD-4409 is an inhibitor of ubiquitin-activating enzyme (UAE, IC50 = 20 µM in a cell-free assay). It decreases levels of ubiquitinated cell division cycle 34 (Cdc34) in K562 chronic myeloid leukemia (CML) cells when used at a concentration of 50 µM. PYZD-4409 increases levels of cyclin D3 and p53 in HCT116 colorectal cancer cells. It selectively reduces colony formation in primary patient-derived acute myeloid leukemia (AML) cells over primary human hematopoietic cells when used at a concentration of 10 µM. PYZD-4409 (10 mg/kg) decreases tumor weight in an MDAY-D2 murine lymphoma model. InChI: InChI=1S/C14H7ClFN3O5/c15-10-5-7(1-3-11(10)16)18-14(21)9(13(20)17-18)6-8-2-4-12(24-8)19(22)23/h1-6H,(H,17,20) InChIKey: MSYMKEYWUWVZQY-UHFFFAOYSA-N SMILES: ClC1=CC(N(NC2=O)C(C2=CC3=CC=C([N+]([O-])=O)O3)=O)=CC=C1F