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C646

SKU: orb1305465

Description

C646 is a potent, selective, and competitive inhibitor of the histone acetyltransferase p300 (Ki=400 nM). It functions as an apoptosis inducer and radiosensitizer, with research applications in oncology for studying epigenetic mechanisms in both cellular and animal models.

Research Area

Cell Biology, Epigenetics & Chromatin

Images & Validation

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C646

Key Properties

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CAS Number328968-36-1
MW445.42
Purity99.21% (May vary between batches)
FormulaC24H19N3O6
SMILESCC1=NN(C(=O)C1=Cc1ccc(o1)-c1cc(C)c(C)cc1[N+]([O-])=O)c1ccc(cc1)C(O)=O
TargetHistone Acetyltransferase,Autophagy,Apoptosis,Epigenetic Reader Domain
SolubilityDMSO:18.5 mg/mL (41.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:0.45 mg/mL (1.01 mM)

Bioactivity

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Target IC50
p300/CBP:400 nM (Ki)
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.
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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.
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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)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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EpigeneticReaderDomain, Epigenetic Reader Domain, HistoneAcetyltransferase, Histone Acetyltransferase, HATs, HAT, inhibit, Inhibitor, C646, C-646, C 646, Autophagy, Apoptosis, p300/CBP

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  • C646

    C646 [orb1225298]

    >98% (HPLC)

    328968-36-1

    445.42

    C24H19N3O6

    5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 2 mg, 1 g, 500 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
2871948 ↗

Key Properties

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No computed properties available.

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C646 (orb1305465)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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2 mg
$ 90.00
1 ml x 10 mM (in DMSO)
$ 110.00
5 mg
$ 110.00
10 mg
$ 140.00
25 mg
$ 250.00
50 mg
$ 440.00
100 mg
$ 640.00
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