GSK-LSD1 DIHYDROCHLORIDE FUNDAMENTALS EXPLAINED

TAK-243 preferentially bound to UBA1 more than the associated E1 enzymes UBA2, UBA3, and UBA6 in intact AML cells. Inhibition of UBA1 with TAK-243 lowered amounts of ubiquitylated proteins, greater markers of proteotoxic tension and DNA harm anxiety. In vivo, TAK-243 lowered leukemic stress and specific leukemic stem cells with no proof of toxicity