THIAMET G - AN OVERVIEW

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TAK-243 preferentially certain to UBA1 above the associated E1 enzymes UBA2, UBA3, and UBA6 in intact AML cells. Inhibition of UBA1 with TAK-243 lowered amounts of ubiquitylated proteins, enhanced markers of proteotoxic strain and DNA damage strain. In vivo, TAK-243 minimized leukemic load and focused leukemic stem cells with out proof of toxicity.