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-4-57 Hydrochloride is a ligand to the CBFß. AI-4-57 Hydrochloride is a modest potency inhibitor of the binding of wildtype CBFß to the RUNX1 Runt domain.
WUN40378 is compound first reported in PCT Int. Appl. (2019), WO 201909959, in which it was described as CBFβ-RUNX1 inhibitor. WUN40378 is very similar to Ro 5-3335 but with an F instead of Cl. WUN40378 is also analog of Ro 24-7429. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https: www.medkoo.com page naming).