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C646

Catalog No. T2452 CAS 328968-36-1

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

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C646, CAS 328968-36-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 206.00
50 mg	In stock	$ 400.00
100 mg	In stock	$ 592.00
500 mg	In stock	$ 1,270.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.21%

Purity: 99%

Purity: 98%

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Description	C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
Targets&IC50	p300/CBP:400 nM(Ki)
In vitro	In the spinal cord, C646 can attenuate mechanical and thermal hyperalgesia, accompanied by the suppression of COX-2 expression. When administered immediately after weak extinction training into the ILPFC, C646 enhances the integration of fear extinction memory.
In vivo	In vitro, C646 at a concentration of 10 μM inhibits p300 by 86%. In castration-sensitive androgen-responsive prostate cancer cell lines, C646 (20 μM) induces apoptosis by interfering with the AR and NF-kB pathways. Furthermore, C646 at 25 μM reduces the acetylation levels of histones H3 and H4 and blocks TSA-induced acetylation. In mouse cells, C646 inhibits the dynamic acetylation of all H3K4me3, spanning locally across promoters and transcription start sites of inducible genes, thereby disrupting the interaction with RNA polymerase II and the activation of these genes.
Kinase Assay	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, 80 μM EDTA, 40μg/ml BSA, 100 μM 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.
Cell Research	Histone acetylation assays in mouse cells. C3H10T1/2 mouse fibroblasts are grown in DMEM with 10% FCS at 37°C with 6% CO2. Confluent cultures are rendered quiescent in DMEM with 0.5% FCS for 18-20 hr prior to treatment. Cells are treated with the following compounds: TSA (10 ng/ml [33 nM]), C646 (25 μM), C37 (25 μM). Antibodies are used at the following concentrations: total H3 (1:10000; ab7834; Abcam); H4K12ac (1:2500; 06-761; Upstate). Rabbit anti-H3K9ac (1:10000) antibodies are generated in-house. Histones are isolated from cells by acid extraction, separated by SDS and acid-urea polyacrylamide gel electrophoresis and analyzed by western blotting.(Only for Reference)

Molecular Weight	445.42
Formula	C24H19N3O6
CAS No.	328968-36-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.45 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. Bowers EM, et al. Chem Biol, 2010, 17(5), 471-482. 2. Santer FR, et al. Mol Cancer Ther, 2011, 10(9), 1644-1655. 3. Crump NT, et al. PNAS, 2011, 108(19), 7814-7819. 4. Marek R, et al. J Neurosci, 2011, 31(20), 7486-7491. 5. Zhu XY, et al. Mol Pain, 2012, 8(84)

Citations

1. Wang S, Lin Y, Gao L, et al. PPAR-γ integrates obesity and adipocyte clock through epigenetic regulation of Bmal1. Theranostics. 2022, 12(4): 1589. 2. Yu G, Chen W, Li X, et al. TWIST1-EP300 Expedites Gastric Cancer Cell Resistance to Apatinib by Activating the Expression of COL1A2. Analytical Cellular Pathology. 2022, 2022. 3. Pan X, Zhang W, Wang L, et al.KLF12 transcriptionally regulates PD‐L1 expression in non‐small cell lung cancer.Molecular Oncology.2023 4. Liang G, He Z, Peng H, et al.Cigarette smoke extract induces the senescence of endothelial progenitor cells by upregulating p300.Tobacco Induced Diseases.2023, 21.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Covalent Inhibitor Library Apoptosis Compound Library Anti-Hypertension Compound Library Reprogramming Compound Library Autophagy Compound Library Anti-Aging Compound Library Target-Focused Phenotypic Screening Library Histone Modification Compound Library

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Keywords

C646 328968-36-1 Apoptosis Autophagy Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase Inhibitor C-646 HATs C 646 HAT inhibit inhibitor

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