DETAILS, FICTION AND PRT062607 HYDROCHLORIDE

TAK-243 preferentially sure to UBA1 over the associated E1 enzymes UBA2, UBA3, and UBA6 in intact AML cells. Inhibition of UBA1 with TAK-243 diminished amounts of ubiquitylated proteins, amplified markers of proteotoxic worry and DNA destruction stress. In vivo, TAK-243 lowered leukemic burden and targeted leukemic stem cells with out evidence of t