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 7 Publications
5 Customer Reviews
Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
Sci Rep, 2016, 6:24838.. C646 purchased from Selleck.
A. Immunoprecipitation of HSP90 from NT, shHSF1 or shHSF1 Mec-1 cells treated with 20 μM, C646 for 24 hours followed by immunoblotting for acetyl lysine and HSP90 (top panel). Immunoprecipitation of CDC37 followed by immunoblot analysis of HSP90 and the indicated HSP90 client kinases (bottom panel).
Oncotarget, 2015, 6(31):31767-79.. C646 purchased from Selleck.
The expression of Dtprp in stromal cells at 96 h decreased in a dose-dependent manner when stromal cells were treated with histone acetyltransferase inhibitor C646.
Biol Reprod, 2015, 93(1): 13. C646 purchased from Selleck.
Left: The protein level of acH4K5 in the DMSO and C646 5 µM groups. H4 was used as a loading control. Right: The expression level of cyclin D3 decreased in the C646 5 µM group compared with the DMSO group detected by Western blotting analysis. Protein lysates for Western blot analysis were obtained at 48 h after C646 treatment.
Biol Reprod, 2015, 93(1): 13. C646 purchased from Selleck.
C646 attenuates ETV1 expression and inactivates KIT-dependent pathways. GIST882 cells were treated with C646 (5-20 μmol/l) for 24 h. Imatinib (500 nmol/l) alone or in combination with C646 (15 μmol/l) was used for the combination study. DMSO was used as the vehicle control. The expression levels of ETV1 and KIT-dependent pathway-related proteins were analysed by western blotting. GAPDH was used as a reference. ETV1, ETS translocation variant 1; GIST, gastrointestinal stromal tumor; DMSO, dimethyl sulfoxide; GAPDH, glyceraldehyde 3-phosphate dehydrogenase.
Oncol Rep, 2016, 36(5):2763-2770.. C646 purchased from Selleck.
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Choose Selective Histone Acetyltransferase Inhibitors
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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||5% DMSO+30% PEG 300+ddH2O||1mg/mL|
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