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C 646
- Moderately soluble in DMSO
- MF: C24H19N3O6
- MW: 445.42
Description
C 646 is a competitive p300/CBP histone acetyltransferase (HAT) inhibitor with a Ki value of 400 nM.
p300 and CBP acetyltransferases regulate histone acetylation, enhancer activity and transcriptional coactivation. C 646 is used to study acetyltransferase-dependent transcription and epigenetic regulation with selectivity versus other acetyltransferases.
Key Features
- Competitive inhibitor of p300/CBP HAT activity
- Ki: 400 nM
- Selective versus other acetyltransferases
- Modulates histone acetylation and transcriptional coactivation
Applications
- p300/CBP enzyme assays
- Histone acetylation and chromatin research
- Transcriptional coactivator studies
- Epigenetic inhibitor selectivity profiling
More Information
| Parent CAS No. | 328968-36-1 |
|---|---|
| Chemical Name | 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid |
| SMILES | C1C(N2N=C(C)C(=CC3=CC=C(C4C([N+]([O-])=O)=CC(C)=C(C)C=4)O3)C2=O)=CC=C(C(O)=O)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30) |
| InChiKey | HEKJYZZSCQBJGB-UHFFFAOYSA-N |
| CID | 1285941 |
| Short Description | p300 HAT inhibitor |
References
- EM Bowers et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem. Biol. 2010, 17, 471-482. [onlne]
- NY Crump et al. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc Natl Acad Sci U S A. 2011, 108(19), 7814-7819.
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