TDZD-8 acts as a noncompetitive inhibitor of ATP or GS-1 binding. TDZD-8 shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. TDZD-8 specifically induces cell death of primary leukemia specimens. TDZD-8 ablates leukemia progenitor and stem cells. TDZD-8 treatment induces oxidative stress. TDZD-8 induces cell death with extremely rapid cell death kinetics showing loss of membrane integrity. TDZD-8 inhibits PKC and FLT3 in primary AML specimens.