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Submit ReviewEPZ 004777 is a highly potent DOT1L inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for DOT1L over a panel of other methyltransferases. Selectively inhibits proliferation and induces apoptosis of MLL-rearranged cells in vitro. Prolongs survival in a MLL xenograft mouse model. Enhances efficiency of Yamanaka-factor factor reprogramming of fibroblasts by 3-4-fold.
For more information about how EPZ 004777 may be used, see our protocol:
Highly Efficient Generation of CiPSCs from MEFsSold under license from Epizyme, Inc.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of EPZ004777 is reviewed on the chemical probes website.
EPZ 004777 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 539.67 |
公式 | C28H41N7O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1338466-77-5 |
PubChem ID | 56962336 |
InChI Key | WXRGFPHDRFQODR-ICLZECGLSA-N |
Smiles | NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3)C=C2)=NC=N1 |
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 | 53.97 | 100 | |
ethanol | 53.97 | 100 |
以下数据基于产品分子量 539.67。 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 | 1.85 mL | 9.26 mL | 18.53 mL |
5 mM | 0.37 mL | 1.85 mL | 3.71 mL |
10 mM | 0.19 mL | 0.93 mL | 1.85 mL |
50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
参考文献是支持产品生物活性的出版物。
Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418
Onder et al (2012) Chromatin-modifying enzymes as modulators of reprogramming. Nature 483 598 PMID: 22388813
If you know of a relevant reference for EPZ 004777, please let us know.
关键词: EPZ 004777, EPZ 004777 supplier, EPZ004777, highly, potent, DOT1L, methyltransferases, histones, inhibitors, inhibits, HMTs, MLL, leukemia, mll-rearranged, H3K79me, Lysine, Methyltransferases, Other, Stem, Cell, Reprogramming, 5567, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 EPZ 004777 的部分引用包括:
Ebrahimi et al (2019) Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming. Nat.Chem.Biol 15 519 PMID: 30962627
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