≥98% ベースライン干渉を最小限に抑える必要がある、感度の高いクロマトグラフィーおよび分析ワークフロー向け。
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Information
EN4 EN4, a covalent ligand that targets cysteine 171 (C171) of MYC , is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
Targets
MYC
In vitro
EN4 directly targets MYC in cells, reduces MYC and MAX thermal stability, inhibits MYC transcriptional activity, downregulates multiple MYC transcriptional targets, and impairs tumorigenesis. EN4 treatment significantly impairs 231MFP breast cancer cell proliferation in a dose- and time-dependent manner. EN4 impairs the cell survival of MYC transformed mammary epithelial MCF10A cells, but not parental MCF10A cells that are not dependent on MYC.
In vivo
EN4 treatment initiated after establishment of a 231MFP breast tumor xenograft in immune-deficient mice also significantly attenuates tumor growth in vivo.
Cell Research(from reference)
Cell lines：231MFP, MDA-MB-231, HEK293T and MCF10A cells
Concentrations：50 μM
Incubation Time：24 h
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| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| 分類 | Benzene and substituted derivatives |
| Subclass | Anilides |
| Intermediate Tree Nodes | Aromatic anilides |
| Direct Parent | Benzanilides |
| Alternative Parents | Diphenylethers Diarylethers Benzamides Phenoxy compounds Phenol ethers Benzoyl derivatives Alkyl aryl ethers Acrylic acids and derivatives Secondary carboxylic acid amides Organonitrogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic homomonocyclic compounds |
| Substituents | Benzanilide - Diphenylether - Diaryl ether - Benzamide - Benzoic acid or derivatives - Phenoxy compound - Benzoyl - Phenol ether - Alkyl aryl ether - Acrylic acid or derivatives - Secondary carboxylic acid amide - Carboxamide group - Carboxylic acid derivative - Ether - Organic nitrogen compound - Organonitrogen compound - Organooxygen compound - Carbonyl group - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Aromatic homomonocyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene. |
| External Descriptors | Not available |
| 溶解度 | Solubility (25°C) In vitro DMSO: 83 mg/mL (199.29 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| 感度 | Light sensitive |
| DMSO（mg / mL） 最大溶解度 | 83 |
| DMSO（mM） 最大溶解度 | 199.294066799529 |
| 水（mg / mL） 最大溶解度 | ＜1 |
| 分子量 | 416.500 g/mol |
| XLogP3 | 4.300 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 9 |
| Exact Mass | 416.174 Da |
| Monoisotopic Mass | 416.174 Da |
| Topological Polar Surface Area | 76.700 Ų |
| Heavy Atom Count | 31 |
| Formal Charge | 0 |
| Complexity | 580.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
F2222581