CAS: 1000874-21-4

KRX 0402 is a methyltransferase inhibitor that competes with the natural substrate, O6-benzylguanine, for binding to the enzyme. KRX 0402 has been shown to inhibit protein synthesis in human leukemia cells and in human cells grown on collagen gels. This drug also has toxicity studies which show it is less toxic than alkylating agents like cyclophosphamide and melphalan. KRX 0402 has been shown to be an effective chemotherapeutic treatment for leukemia cells, because it inhibits DNA synthesis by blocking the activity of key enzymes involved in this process, including topoisomerase II. It may also have an effect on cell growth and differentiation by inhibiting transcription factors such as E2F-1 and stem cell factor (SCF).