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
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M.Wt
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578.46
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Formula
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C28H17F3N4O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(Trifluoromethyl)benzyl 4-(6-(2,6-dihydroxy-3-nitrobenzoyl)pyrazolo[1,5-a]pyrimidin-2-yl)benzoate
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References
1. Ying-Zhe Wang, et al. J Med Chem. 2023 Dec 14;66(23):15944-15959.
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