CHS-828 NEW
| Price | $50 | $79 | $165 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: CHS-828 | CAS No.: 200484-11-3 |
| Purity: 99.76% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | 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 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. [1] GMX1778 induces programmed cell death with apoptotic features. [2] GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM). [3] |
| 體內(nèi)活性 | GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice. [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 |
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| 相關(guān)庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 抗代謝疾病化合物庫(kù) | 抗癌活性化合物庫(kù) | 抗癌藥物庫(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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