C646, p300/CBP inhibitor


Catalog No. size PriceQuantity
M60129-2D 10 mM in DMSO (0.449 mL) $129
M60129-2S 2 mg solid $129
M60129-10S 10mg solid $535

Description

Product Information
Molecular Weight: 445.42
Formula: C24H19N3O6
Purity: ≥98%
CAS#: 328968-36-1
Solubility: DMSO up to 30 mM
Chemical Name: (Z)-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
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 


Biological Activity:

C646 is a potent, selective and cell-permeable p300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 ~400 nM. It competes with acetyl-CoA for the p300 Lys-CoA binding pocket selectively. It blocks the growth of human melanoma, leukemia, lung, and prostate cancer cells in vitro. C646 has also been used to study the role of p300-mediated gene regulation in neuroscience. The histone acetyltransferase (HAT) p300/CBP is a transcriptional coactivator implicated in many gene regulatory pathways and protein acetylation events. C646 is a useful chemical probe to study p300/CBP HAT functions. 

 

How to Use:

In vitro:  C646 was used at 10 µM final concentration in various in vitro assays.

In vivo: C646 was dosed to mice by Alzet pumps at 0.9 mg/kg per day for 14 days.

 

Reference:

 

  1.  Gao XN, et al. A histone acetyltransferase p300 inhibitor C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells. (2013) PLoS One. 8(2):e55481
  2.  Santer FR, et al. Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines. (2011) Mol Cancer Ther. 10(9):1644-55.
  3.  Crump NT, et al. Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP. (2011) Proc Natl Acad Sci USA. 108(19):7814-9.
  4.  Marek R, et al. Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300. (2011) J Neurosci. 31(20):7486-91.
  5. Bowers EM, et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. (2010) Chem Biol. 17(5):471-82. 
Products are for research use only. Not for human use.

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