價(jià)格 | ¥193 | ¥412 | ¥661 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱(chēng):化合物 CHS 828 | 英文名稱(chēng):CHS-828 |
CAS:200484-11-3 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.76% | 產(chǎn)品類(lèi)別: 抑制劑 |
貨號(hào): T1998 |
名稱(chēng) | CHS-828 |
描述 | CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM). |
細(xì)胞實(shí)驗(yàn) | Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values.(Only for Reference) |
激酶實(shí)驗(yàn) | In vitro coupled-enzyme NAMPT assay: Recombinant NAMPT activity is assessed using a coupled-enzyme assay based on the quantitation of NAD+. Reactions are performed at room temperature for 180 min using mixtures consisting of 50 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 0.5 mM β-mercaptoethanol, 0.005% bovine serum albumin, 1% DMSO, 2.0 U/ml lactate dehydrogenase, 4 mM sodium L-lactate, 0.4 U/ml diaphorase, 6 μΜ resazurin sodium salt, 0.4 mM PRPP, 3.0 nM NMNAT1, 125 μM ATP, 50 μM NM, and 2 to 5 μM recombinant NAMPT. Fluorescence s measured with a Tecan Safire plate reader (excitation wavelength, 560 nm; emission wavelength, 590 nm). Ki values are calculated using Graphpad Prism 4.0 software and the Cheng-Prusoff equation. |
體外活性 | GMX1778通過(guò)抑制NAD+的生物合成引起NAD+耗盡,進(jìn)而導(dǎo)致ATP耗竭并最終導(dǎo)致細(xì)胞死亡。[1] GMX1778誘導(dǎo)具有凋亡特征的程序性細(xì)胞死亡。[2] GMX1778通過(guò)下調(diào)IKK活性(IC50=8 nM)抑制癌細(xì)胞中的核因子-κB活性。[3] |
體內(nèi)活性 | GMX1778(250 mg/kg,p.o.)對(duì)于移植至裸鼠的三種不同人類(lèi)神經(jīng)內(nèi)分泌腫瘤——中腸類(lèi)癌(GOT1)、胰腺類(lèi)癌(BON)和甲狀腺髓樣癌(GOT2)——展現(xiàn)了顯著的抗腫瘤活性。[4] |
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 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 69 mg/mL (185.6 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | Nicotinamide phosphoribosyl transferase | CHS828 | NAMPT | inhibit | PBEF | Visfatin | Apoptosis | Inhibitor | GMX 1778 | Pre-B cell colony enhancing factor | GMX-1778 | CHS-828 |
相關(guān)產(chǎn)品 | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
相關(guān)庫(kù) | 抑制劑庫(kù) | 抗癌活性化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 臨床期小分子藥物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 抗癌藥物庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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