Bcl-2-IN-22 (compound 1) is a gold(I) NHC complex with anticancer activity. Bcl-2-IN-22 induces apoptosis via the mitochondrial pathway with an IC 50 value of 0.014 μM. In addition, Bcl-2-IN-22 targets BCL-2 family members and exhibits pro-apoptosis and resensitization properties in multidrug-resistant leukemia cells that overexpress BCL-2.