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DDO-2728

Chemical Structure : DDO-2728

CAS No.: 3029515-97-4

DDO-2728 (DDO 2728)

Catalog No.: PC-22677Not For Human Use, Lab Use Only.

DDO-2728 is a selectiv, 2-OG independent inhibitor of mRNA m6A demethylase AlkB homologue 5 (ALKBH5) with IC50 of 2.97 uM in FP assays, does not inhibit FTO (ALKBH9) and ALKBH3.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DDO-2728 is a selectiv, 2-OG independent inhibitor of mRNA m6A demethylase AlkB homologue 5 (ALKBH5) with IC50 of 2.97 uM in FP assays, does not inhibit FTO (ALKBH9) and ALKBH3.
DDO-2728 directly binds to ALKBH5 with KD of 6.62 uM, but not FTO.
DDO-2728 does not bind to the 2-OG pocket.
DDO-2728 increases m6A methylation levels in the MOLM-13 cells and exhibits antiproliferation activity in AML cells with IC50 of 0.45 and 1.2 uM for MOLM-13 and MV4–11 cells respectivey.
DDO-2728 targets ALKBH5-TACC3 signaling axis, significantly reduces the abundance of TACC3 and c-Myc at both the mRNA and protein levels in MOLM-13 and MV4–11 cells.
DDO-2728 (10 mg/kg, i.p.) significantly inhibited tumor growth in MV4–11 xenograft tumor model.

Physicochemical Properties

M.Wt 578.46
Formula C28H17F3N4O7
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

4-(Trifluoromethyl)benzyl 4-(6-(2,6-dihydroxy-3-nitrobenzoyl)pyrazolo[1,5-a]pyrimidin-2-yl)benzoate

References

1. Ying-Zhe Wang, et al. J Med Chem. 2023 Dec 14;66(23):15944-15959.

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