EP652 | METTL3 inhibitor | Probechem Biochemicals

Chemical Structure : EP652

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EP652 (EP-652)

货号: PC-24016Not For Human Use, Lab Use Only.

EP652 is a potent, selective and in vivo active inhibitor of RNA methyltransferase METTL3 with IC50 of 2 nM (METTL3/14) in SPA primary assays.

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生物&药学活性

EP652 is a potent, selective and in vivo active inhibitor of RNA methyltransferase METTL3 with IC50 of 2 nM (METTL3/14) in SPA primary assays.
EP652 dispalys high selectivity (at 10 μM) against a panel of 40 methyltransferases, as well as in a standard safety screen panel (44 targets, including GPCRs, ion channels, and kinases).
EP652 exhibits m6A inhibition in mRNA from Calu-6 after 24 h treatment with IC50 of 8.6 nM.
EP652 demonstrates potent efficacy in cellulo across various cell lines in Kasumi-1 and MV-4–11 (AML cell lines), Caov-3 and SK-OV-3 (ovarian cancer cell lines), Calu-6 and A549 (lung cancer cell lines), and FaDu (Head and neck cancer cell line)) in cell viability experiments.
EP652 demonstrates dose-dependent decrease of the m6A cellular level in PBMC from rates, maximum m6A reduction (∼75%) at as low as 0.3 mg/kg.
EP652 (10 and 30 mg/kg ip, QD) effectively arrested cancer progression in MV-4-11 model (MV-4-11-Luc-mCh-Puro CDX model).

物理化学性质&存储条件

分子量	462.60
分子式	C25H34N8O
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-((R)-3-((Cyclopropylmethyl)amino)piperidin-1-yl)-1-((R)-1-(4-(5-(dimethylamino)pyridin-3-yl)-1H-1,2,3-triazol-1-yl)ethyl)pyridin-2(1H)-one

参考文献

1. Dutheuil G, et al. J Med Chem. 2025 Feb 13;68(3):2981-3003.

EP652 (EP-652)

生物&药学活性

物理化学性质&存储条件

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EP652 (EP-652)

生物&药学活性

物理化学性质&存储条件

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