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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H19N3O6 |
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分子量 | 445.42 | CAS No. | 328968-36-1 | |
Solubility (25°C)* | 体外 | DMSO | 23 mg/mL (51.63 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
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. |
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in vitro | 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. [1] C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. [2] 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. [3] |
in vivo | C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. [4] C646 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. |
キナーゼアッセイ | Radioactive assay | |
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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), 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. | |
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 |
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]
Musashi-2 potentiates colorectal cancer immune infiltration by regulating the post-translational modifications of HMGB1 to promote DCs maturation and migration [ Cell Commun Signal, 2024, 22(1):117] | PubMed: 38347600 |
LINC00355 promotes gastric carcinogenesis by scaffolding p300 to activate CDC42 transcription and enhancing HNRNPA2B1 to stabilize CDC42 mRNA dependent on m6A [ Mol Carcinog, 2024, 63(3):430-447] | PubMed: 37983727 |
NINJ1 regulates ferroptosis via xCT antiporter interaction and CoA modulation [ bioRxiv, 2024, 2024.02.22.581432] | PubMed: 38464226 |
METTL14 Promotes Lipid Metabolism Reprogramming and Sustains Nasopharyngeal Carcinoma Progression via Enhancing m6A Modification of ANKRD22 mRNA [ Research Square, 2024, 10.21203/rs.3.rs-3834927/v1] | PubMed: none |
Noncanonical CDK4 signaling rescues diabetes in a mouse model by promoting β cell differentiation [ J Clin Invest, 2023, 133(18)e166490] | PubMed: 37712417 |
Hepatocyte HSPA12A inhibits macrophage chemotaxis and activation to attenuate liver ischemia/reperfusion injury via suppressing glycolysis-mediated HMGB1 lactylation and secretion of hepatocytes [ Theranostics, 2023, 13(11):3856-3871] | PubMed: 37441587 |
Noncanonical CDK4 signaling rescues diabetes in a mouse model by promoting β cell differentiation [ J Clin Invest, 2023, 133(18)e166490] | PubMed: 37712417 |
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602] | PubMed: 37148583 |
Lactate promotes myogenesis via activating H3K9 lactylation-dependent up-regulation of Neu2 expression [ J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363] | PubMed: 37919243 |
A regulatory circuit comprising the CBP and SIRT7 regulates FAM134B-mediated ER-phagy [ J Cell Biol, 2023, 222(5)e202201068] | PubMed: 37043189 |
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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