Molecular Weight(MW): 445.42
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases.
Cited by 32 Publications
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Choose Selective Histone Acetyltransferase Inhibitors
|Description||C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases.|
|Features||Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.|
C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a Ki of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells.  C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways.  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 these genes. 
|In vivo||C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory.  C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord. |
Radioactive assay:IC50 values for the putative p300 HAT inhibitors are determined using the direct radioactive assay described above. Reactions are performed in 20 mM HEPES (pH 7.9), and contained 5 mM DTT, 80μM EDTA, 40μg/ml BSA, 100μM H4-15, and 5 nM p300. Putative inhibitors are added over a range of concentrations, with DMSO concentration kept constant (<5%). Reactions are incubated at 30°C for 10 min, then initiated with addition of a 1:1 mixture of 12C-acetyl-CoA and 14C-acetyl-CoA to 20 mM. After 10 min at 30°C, reactions are quenched with 14% SDS (w/v). All concentrations are screened in duplicate. Gels are run, washed, dried, and exposed to a PhosphorImager plate, and production of Ac-H4-15 quantified to obtain IC50s.
|In vitro||DMSO||13 mg/mL (29.18 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5%Tween 80+ddH2O
For best results, use promptly after mixing.
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Frequently Asked Questions
I am planning to conduct IP studies in mice, any specific vehicle that you can recommend to me?
We found it can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 1 mg/ml as a clear solution. It should be ok for i.p. injection.