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C646

Chemical Structure : C646

CAS No.: 328968-36-1

C646 (p300 inhibitor C646)

Catalog No.: PC-20778Not For Human Use, Lab Use Only.

C646 is a selective, competitive histone acetyltransferase (HAT) p300 inhibitor with Ki of 400 nM, less potent for other acetyltransferases.

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Biological Activity

C646 is a selective, competitive histone acetyltransferase (HAT) p300 inhibitor with Ki of 400 nM, less potent for other acetyltransferases.
C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of genes.
C646 increses caspase-dependent apoptosis involving both extrinsic and intrinsic cell death pathways in androgen-dependent and castration-resistant prostate cancer cells.
C646 inhibits the growth of human melanoma and other tumor cells and promotes cellular senescence.

Physicochemical Properties

M.Wt 445.42
Formula C24H19N3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid

References

1. Bowers EM, et al. Chem Biol. 2010 May 28;17(5):471-82.

2. Yan G, et al. J Invest Dermatol. 2013 Oct;133(10):2444-2452.

3. Santer FR, et al. Mol Cancer Ther. 2011 Sep;10(9):1644-55.

4. Crump NT, et al. Proc Natl Acad Sci U S A. 2011 May 10;108(19):7814-9.

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