DMI46 (DMI-46)

Chemical Structure : DMI46

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货号: PC-26538Not For Human Use, Lab Use Only.

DMI46 (DMI-46) is a potent, selective inhibitor of DNA methyltransferase 1 (DNMT1) with enzymetic IC50 of 7.9 nM, reverses cancer-specific DNA methylation abnormalities and tumor suppressor genes (TSGs) silencing, leading to robust antileukemic effects.

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生物&药学活性

DMI46 (DMI-46) is a potent, selective inhibitor of DNA methyltransferase 1 (DNMT1) with enzymetic IC50 of 7.9 nM, reverses cancer-specific DNA methylation abnormalities and tumor suppressor genes (TSGs) silencing, leading to robust antileukemic effects.

DMI46 robustly derepresses the DNA hypermethylated TSG reporter at sub-100 nM concentrations (EC50 = 62.70 nM).

DMI46 exhibits approximately threefold greater enzymatic DNMT1 inhibition than GSK3685032 (GSK5032, IC50=22.57 nM).

DMI46 reverses promoter DNA hypermethylation and associated TSG silencing, suppressing AML growth both in vitro and in vivo.

DMI46 also significantly inhibits the proliferation of colon and lung cancer cells, with IC50 values of roughly 100 to 300 nM in HCT116 and RKO CRC cells that display abnormal gene promoter CpG island methylator phenotypes (CIMPs).

DMI46 exhibits moderately reduced growth inhibitory activity against GSK5032-resistant AML cells.

DMI46 exerts potent antiproliferative effects against DAC-resistant AML cells both in vitro and in vivo.

物理化学性质&存储条件

分子量	533.65
分子式	C27H31N7O3S
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)-2-(6-((2-amino-1-(4-methoxyphenyl)-2-oxoethyl)thio)-3,5-dicyano-4-ethyl-1H-pyrrolo[2,3-b]pyridin-1-yl)-N-(2-(dimethylamino)ethyl)-N-methylacetamide

参考文献

1. Tang S, et al. Proc Natl Acad Sci U S A. 2026 Apr 14;123(15):e2532472123.

DMI46 (DMI-46)

生物&药学活性

物理化学性质&存储条件

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DMI46 (DMI-46)

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物理化学性质&存储条件

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