Chemical Structure : DDO-2728
CAS No.: 3029515-97-4
货号: PC-22677Not For Human Use, Lab Use Only.
DDO-2728 is a selective, 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.
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥880 | In stock | |
| 10 mg | ¥1280 | In stock | |
| 25 mg | ¥2180 | In stock | |
| 50 mg | ¥3580 | In stock | |
| 100 mg | Get quote |
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DDO-2728 is a selective, 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.
| 分子量 | 578.46 | |
| 分子式 | C28H17F3N4O7 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-(Trifluoromethyl)benzyl 4-(6-(2,6-dihydroxy-3-nitrobenzoyl)pyrazolo[1,5-a]pyrimidin-2-yl)benzoate |
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1. Ying-Zhe Wang, et al. J Med Chem. 2023 Dec 14;66(23):15944-15959.
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