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RUNX1/ETO inhibitor 7.44

Chemical Structure : RUNX1/ETO inhibitor 7.44

CAS No.: 88755-39-9

RUNX1/ETO inhibitor 7.44

Catalog No.: PC-49279Not For Human Use, Lab Use Only.

RUNX1-ETO inhibitor 7.44 is a first-in-class, small-molecule inhibitor of RUNX1/ETO tetramerization, specifically interferes the nervy homology region 2 (NHR2) domain of ETO mediating tetramerization with Klig value of 3.75 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RUNX1-ETO inhibitor 7.44 is a first-in-class, small-molecule inhibitor of RUNX1/ETO tetramerization, specifically interferes the nervy homology region 2 (NHR2) domain of ETO mediating tetramerization with Klig value of 3.75 uM.
RUNX1-ETO inhibitor 7.44 targets the interaction between the NHR2 domain of RUNX1/ETO, interferes with NHR2 tetramer stability and leads to an increase in the dimer population of NHR2.
RUNX1-ETO inhibitor 7.44 binds with both heteroaromatic moieties to NHR2 and interacts with or leads to conformational changes in the N-termini of the NHR2 tetramer.
RUNX1-ETO inhibitor 7.44 has favorable physicochemical, pharmacokinetic, and toxicological properties, shows anti-leukemic effects.

Physicochemical Properties

M.Wt 342.303
Formula C18H14O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,4-bis(benzo[d][1,3]dioxol-5-yl)-4-oxobutanoic acid

References

1. Mohanraj Gopalswamy, et al. Sci Rep. 2022 Aug 19;12(1):14158.

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