C646

製品コードS7152 バッチS715204

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H19N3O6
分子量 445.42 CAS No. 328968-36-1
Solubility (25°C)* 体外 DMSO 11 mg/mL (24.69 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.000mg/ml (2.25mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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. C646 induces cell cycle arrest, apoptosis and autophagy.
in vitro C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a Ki of 400 nM and is selective versus other acetyltransferases. This compound produces 86% inhibition of p300 in vitro at 10 μM. It is a classical reversible p300 inhibitor. This chemical treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. [1] It (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. [2] This compound 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. [3]
in vivo C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. [4] This compound attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord. [5]
特徴 Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 C3H10T1/2
濃度 ~25 μM
反応時間 1 to 3 hr
実験の流れ 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), this compound (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.
動物実験 動物モデル mouse
投薬量 2×0.75 μl injection volume in each case, 1.5 μg, administered over 2 min
投与方法 infusion into ILPFC

参考

  • https://pubmed.ncbi.nlm.nih.gov/20534345/
  • https://pubmed.ncbi.nlm.nih.gov/21709130/
  • https://pubmed.ncbi.nlm.nih.gov/21518915/
  • https://pubmed.ncbi.nlm.nih.gov/21593332/
  • https://pubmed.ncbi.nlm.nih.gov/23176208/

カスタマーフィードバック

Data from [Data independently produced by , , Sci Rep, 2016, 6:24838.]

Data from [Data independently produced by , , Oncotarget, 2015, 6(31):31767-79.]

Data from [Data independently produced by , , Front Neurosci, 2018, doi:10.3389/fnins.2018.00341]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

TIGIT deficiency promotes autoreactive CD4+ T-cell responses through a metabolic‒epigenetic mechanism in autoimmune myositis [ Nat Commun, 2025, 16(1):4502] PubMed: 40374622
Alleviation of liver fibrosis by inhibiting a non-canonical ATF4-regulated enhancer program in hepatic stellate cells [ Nat Commun, 2025, 16(1):524] PubMed: 39789010
Extracellular Histones as Exosome Membrane Proteins Regulated by Cell Stress [ J Extracell Vesicles, 2025, 14(2):e70042] PubMed: 39976275
Loss of p300 in proximal tubular cells reduces renal fibrosis and endothelial-mesenchymal transition [ EMBO Mol Med, 2025, 17(7):1575-1598] PubMed: 40588562
Lactylation modification of HIF-1α enhances its stability by blocking VHL recognition [ Cell Commun Signal, 2025, 23(1):364] PubMed: 40760493
Herbal-based Xuebijing injection ameliorated vascular endothelial dysfunction via inhibiting ACLY/MYB/RIG-I axis in sepsis-associated lung injury [ Phytomedicine, 2025, 140:156573] PubMed: 40088739
Nuclear PD-L1 triggers tumour-associated inflammation upon DNA damage [ EMBO Rep, 2025, 10.1038/s44319-024-00354-9] PubMed: 39747659
Histone acetylation facilitates multidirectional pulp repair through Neuregulin-1 mobilization [ Stem Cells Transl Med, 2025, 14(7)szaf022] PubMed: 40580029
Matrix stiffness induced gallbladder fibroblasts activation and paracrine SEMA7A promotes gallbladder cancer cell epithelial-mesenchymal transition and cancer stem cell-like properties by modulating AKT/p300 signalling [ Biol Direct, 2025, 20(1):93] PubMed: 40830485
Knockdown of ACC1 promotes migration and invasion of U251 glioma cells by epigenetically suppressing SDH [ Int J Oncol, 2025, 67(3)73] PubMed: 40747663

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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