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C 646

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C 646 | CAS No. 328968-36-1 | Other Transferase Inhibitors
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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%

Product Details
Reviews (1)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

C 646 is a 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. Also represses pluripotency markers in mouse embryonic stem cells.

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

Technical Data

M.Wt:
445.42
Formula:
C24H19N3O6
Solubility:
Soluble to 25 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
328968-36-1

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.

Additional Information

Other Product-Specific Information:
  • This compound is a mixture of Z:E isomers (~ 80:20)

Background References

  1. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.
    Bowers et al.
    Chem.Biol., 2010;17:471
  2. Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes.
    Mali et al.
    Stem Cells, 2010;28:713
  3. HAT trick: p300, small molecule, inhibitor.
    Ott and Verdi
    Chem.Biol., 2010;17:417
  4. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP.
    Crump et al.
    Proc.Natl.Acad.Sci. USA, 2011;108:7814
  5. Roles for histone acetylation in regulation of telomere elongation and two-cell state in mouse ES cells.
    Dan et al.
    J.Cell.Physiol., 2015;230:2337

Product Datasheets

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C 646 In vitro concentration
By Anonymous on 01/08/2018
Application: Species: Human

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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