EP102 | METTL3 inhibitor | Probechem Biochemicals

Chemical Structure : EP102

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EP102 (EP-102)

货号: PC-26542Not For Human Use, Lab Use Only.

EP102 is a potent, selective METTL3 inhibitor with IC50 of 2 nM in SPA primary assay.

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生物&药学活性

EP102 is a potent, selective METTL3 inhibitor with IC50 of 2 nM in SPA primary assay.
EP102 showed nanomolar potency across a broad panel of cancer cell lines (Kasumi-1 (IC50=61 nM) and MV-4-11 (AML), Calu-6 and A549 (lung), FaDu (head and neck), and Caov-3 and SK-OV-3 (ovarian)).
EP102 potently inhibits intracellular m6A in SK-OV-3 cells with IC50 of 6 nM,.
EP102 selectively inhibits METTL3/14 among a panel of 40 methyl transferases.
EP102 demonstrated a dose-dependent inhibition of m6A up to a maximum reduction (79%) following a single dose of 3 mg/kg (oral) in PBMCs from rats.
EP102 (20 mg/kg, po, QD) inhibited tumor growth in AML xenograft model (MV-4-11-Luc-mCh-Puro CDX model).

物理化学性质&存储条件

分子量	488.65
分子式	C27H32N6OS
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	(R)-N-(Cyclopropylmethyl)-1-(6-(3-(5-(5-cyclopropylpyridin-3-yl)-1,3,4-thiadiazol-2-yl)oxetan-3-yl)pyridin-3-yl)piperidin-3-amine

参考文献

1. Dutheuil G, et al. J Med Chem. 2026 Apr 13. doi: 10.1021/acs.jmedchem.6c00474.

EP102 (EP-102)

生物&药学活性

物理化学性质&存储条件

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EP102 (EP-102)

生物&药学活性

物理化学性质&存储条件

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