C 646

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Cat.No. 4200 - C 646 | C24H19N3O6 | CAS No. 328968-36-1
Description: Selective p300/CBP inhibitor
Chemical Name: 4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

Selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM). Selective for p300 over six other histone acetyltransferases (HATs). Suppresses histone H3 and H4 acetylation in mouse fibroblast cell lines.

This compound is a mixture of Z:E isomers (~ 80:20).

Compound Libraries

C 646 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 445.42
Formula C24H19N3O6
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 328968-36-1
PubChem ID 1285941
InChI Key HEKJYZZSCQBJGB-UNOMPAQXSA-N
Smiles CC/2=NN(C(C2=C/C3=CC=C(C4=CC(C)=C(C)C=C4[N+]([O-])=O)O3)=O)C1=CC=C(C(O)=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.14 25

Preparing Stock Solutions

The following data is based on the product molecular weight 445.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.25 mM 8.98 mL 44.9 mL 89.8 mL
1.25 mM 1.8 mL 8.98 mL 17.96 mL
2.5 mM 0.9 mL 4.49 mL 8.98 mL
12.5 mM 0.18 mL 0.9 mL 1.8 mL

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References

References are publications that support the biological activity of the product.

Bowers et al (2010) Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem.Biol. 17 471 PMID: 20534345

Mali et al (2010) Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes. Stem Cells 28 713 PMID: 20201064

Ott and Verdi (2010) HAT trick: p300, small molecule, inhibitor. Chem.Biol. 17 417 PMID: 20534339

Crump et al (2011) Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. Proc.Natl.Acad.Sci. USA 108 7814


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Keywords: C 646, C 646 supplier, C646, p300, CREB-binding, proteins, CBP, inhibitors, inhibits, histone, acetyltransferase, hat, kat, posttranslational, modifications, epigenetics, Post-translational, Modifications, Histone, Acetyltransferases, 4200, Tocris Bioscience

Citations for C 646

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Reviews for C 646

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C 646 In vitro concentration
By Anonymous on 01/08/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Intestinal subepithelial myofibroblasts, smooth muscle cells,

It is dissolved well in DMSO. I diluted it with serum free medium (final concentration of 10 micromolar) and treated the cells for different time points to detect its inhibitory effect of p300 at protein level.


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