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RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model[1][2][3].

[1] Metz A, et al. From determinants of RUNX1/ETO tetramerization to small-molecule protein-protein interaction inhibitors targeting acute myeloid leukemia. J Chem Inf Model. 2013 Sep 23;53(9):2197-202. DOI:10.1021/ci400332e
[2] Schanda J, et al. Suppression of RUNX1/ETO oncogenic activity by a small molecule inhibitor of tetramerization. Haematologica. 2017 May;102(5):e170-e174. DOI:10.3324/haematol.2016.161570
[3] Gopalswamy M, et al. Biophysical and pharmacokinetic characterization of a small-molecule inhibitor of RUNX1/ETO tetramerization with anti-leukemic effects. Sci Rep. 2022 Aug 19;12(1):14158. DOI:10.1038/s41598-022-17913-6
[4] Kaoud TS, et al. From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules. ACS Med Chem Lett. 2012 Aug 6;3(9):721-725. DOI:10.1021/ml300129b