EED 226

Pricing Availability   Qty
说明: Potent and selective EED inhibitor
化学名: N-(2-Furanylmethyl)-8-[4-(methylsulfonyl)phenyl]-1,2,4-triazolo[4,3-c]pyrimidin-5-amine
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for EED 226

EED 226 is a potent (IC50 = 23.4 nM) and selective EED inhibitor. It inhibits PRC2 activity by binding to the H3K27me3 pocket of EED. The compound shows selectivity for PRC2 complex over protein methyltransferases, kinases, and other protein classes. In vitro, EED 226 regulates histone H3K27 methylation and PRC2 target gene expression. In vivo, it induces tumor regression in a mouse xenograft model. EED 226 is orally bioavailable.

技术数据 for EED 226

分子量 369.4
公式 C17H15N5O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2083627-02-3
PubChem ID 123132228
InChI Key DYIRSNMPIZZNBK-UHFFFAOYSA-N
Smiles O=S(=O)(C1=CC=C(C=C1)C2=CN=C(NCC=3OC=CC3)N4C=NN=C24)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for EED 226

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 36.94 100

制备储备液 for EED 226

以下数据基于产品分子量 369.4。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.54 mL 27.07 mL
5 mM 0.54 mL 2.71 mL 5.41 mL
10 mM 0.27 mL 1.35 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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参考文献 for EED 226

参考文献是支持产品生物活性的出版物。

Qi et al (2017) An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat.Chem.Biol. 13 381 PMID: 28135235


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关键词: EED 226, EED 226 supplier, EED226, potent, selective, EED, histone, methyltransferase, inhibitors, inhibits, PRC2, polycomb, repressive, complex, 2, orally, bioavailable, Other, Lysine, Methyltransferases, 7762, Tocris Bioscience

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