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C-646 | HAT inhibitor

CAS:
328968-36-1
Catalog Number:
10-1306
Activity:
HAT 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
Molecular Weight:
445.44
Molecular Formula:
C24H19N3O6
Solubility:
Soluble in DMSO (up to 10 mg/ml).
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

C-646 (328968-36-1) is a potent and selective inhibitor of the histone acetyl transferase p300/CBP (Ki=400 nM ). Induces apoptosis in prostate cancer cells. C-646 enhances fear extinction memory and synaptic plasticity in mice. Promotes tau deacetylation reducing levels of pathogenic p-tau. Cell permeable.

References/Citations:

1) Bowers et al. (2010), Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor; Chem. Biol., 17 471
2) Santer et al. (2011), Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines; Mol. Cancer Ther., 10 1644
3) Marek et al. (2011), Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300; J. Neurosci.., 31 7486
4) Min et al. (2010), Acetylation of tau inhibits its degradation and contributes to tauopathy; Neuron, 67 953

C-646 | HAT inhibitor is also available in the Cellular Metabolism Library.
CAS:
328968-36-1
Catalog Number:
10-1306
Activity:
HAT 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
Molecular Weight:
445.44
Molecular Formula:
C24H19N3O6
Solubility:
Soluble in DMSO (up to 10 mg/ml).
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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