C646 NEW
| Price | $41 | $63 | $98 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: C646 | CAS No.: 328968-36-1 |
| Purity: 99.21% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | C646 |
| 描述 | C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay). |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 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. |
| 體內(nèi)活性 | 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. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 4.45 mg/mL (10 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.45 mg/mL (1.01 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. |
| 關(guān)鍵字 | C646 | Histone Acetyltransferase | Inhibitor | C-646 | HATs | C 646 | Autophagy | HAT | inhibit | Epigenetic Reader Domain | Apoptosis |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 組蛋白修飾化合物庫(kù) | 細(xì)胞重編程化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 染色質(zhì)修飾分子庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 共價(jià)抑制劑庫(kù) | 抗高血壓化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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