C 646

Pricing Availability Delivery Time Qty
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
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.

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.

All Tocris products are intended for laboratory research use only.

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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.25 mL 11.23 mL 22.45 mL
5 mM 0.45 mL 2.25 mL 4.49 mL
10 mM 0.22 mL 1.12 mL 2.25 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: C646 p300 CREB-binding proteins CBP inhibitors inhibits histone acetyltransferase hat kat posttranslational modifications epigenetics Histone Acetyltransferases

Citations for C 646

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Literature in this Area

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Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

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Pathways for C 646

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