IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1 (R132H)/IDH2(R140Q) with IC 50 values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis , demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia.