RUNX1/ETO tetramerization-IN-1

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].

Product Specifications

CAS Number

[88755-39-9]

UNSPSC

12352005

Target

RUNX

Related Pathways

Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C(CC(C1=CC=C2OCOC2=C1)=O)C3=CC=C4OCOC4=C3)O

Molecular Formula

C18H14O7

Molecular Weight

342.30

References & Citations

[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. |[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. |[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. |[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.