DC-PRC2in-01 | EZH2-EED inhibitor | Probechem Biochemicals

Chemical Structure : DC-PRC2in-01

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DC-PRC2in-01 (EZH2-EED inhibitor)

货号: PC-20124Not For Human Use, Lab Use Only.

DC-PRC2in-01 is a small molecule PRC2 inhibitor targeting EZH2-EED interaction with affinity Kd of 4.56 uM, decreases global H3K27me3 levels in cancer cells.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

DC-PRC2in-01 is a small molecule PRC2 inhibitor targeting EZH2-EED interaction with affinity Kd of 4.56 uM, decreases global H3K27me3 levels in cancer cells.
DC-PRC2in-01 shows an IC50 of 4.21 μM for bindingt to EED in the fluorescence polarization (FP) competitive binding assays.
DC-PRC2in-01 destabilizes the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells.
DC-PRC2in-01 effectively inhibits the proliferation of PRC2-driven lymphomas cells, arrested the cell cycle in the G0/G1 phase.
DC-PRC2in-01 shows growth inhibition effects on cancer cells, including Pfeiffer, KARPAS422, SU-DHL-4, and DB, via a cell viability assay (IC50s=3.5-10 uM).

物理化学性质&存储条件

分子量	444.55
分子式	C27H29FN4O
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	1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)pyrrolidin-3-yl)-1H-benzo[d]imidazol-2-amine

参考文献

1. Daohai Du, et al. J Med Chem. 2021 Jun 24;64(12):8194-8207.