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.
CAS Number: 328968-36-1
Molecular Weight: 445.42
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
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 30 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
C646 was used at 10 µM final concentration in various in vitro assays.
C646 was dosed to mice by Alzet pumps at 0.9 mg/kg per day for 14 days.
- 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
- 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.
- 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.
Products are for research use only. Not for human use.
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