RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their specific targets. This compound triggers p53-dependent apoptosis and suppresses the proliferation of cancer cells. Furthermore, RUNX-IN-1 has demonstrated efficacy in impeding tumor progression in PANC-1 xenograft mice [1].

RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting cancer cell proliferation and inducing p53-dependent apoptosis. Furthermore, RUNX-IN-2 suppresses tumor development in PANC-1 xenograft mice and demonstrates notable alkylation efficiency and specificity [1].

RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor that specifically targets NHR2 of RUNX1/ETO, effectively inhibiting the tetramerization process. With an EC50 value of 0.25 μM, this compound successfully restores gene expression that has been down-regulated by RUNX1/ETO. Furthermore, RUNX1/ETO tetramerization-IN-1 demonstrates promising anti-leukemic activity by inhibiting the proliferation of SKNO-1 cells dependent on RUNX1/ETO and significantly reducing RUNX1/ETO-associated tumor growth in a mouse model [1] [2] [3].

AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) is a small molecule inhibitor of CBFβ-RUNX binding(IC50 : 3.2 μM).