DDO-2728 | ALKBH5 inhibitor | Probechem Biochemicals

Chemical Structure : DDO-2728

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DDO-2728 (DDO 2728)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	578.46
分子式	C28H17F3N4O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

DDO-2728 (DDO 2728)

生物&药学活性

物理化学性质&存储条件

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DDO-2728 (DDO 2728)

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物理化学性质&存储条件

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