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Submit ReviewEED 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.94 | 100 |
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.
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 |
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
If you know of a relevant reference for EED 226, please let us know.
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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