化合物CHS 828 T1998

Product Introduction
Bioactivity


英文名: CHS-828

描述: CHS-828 (GMX1778) 是一种竞争性的烟酰胺磷酸化转移酶抑制剂，IC50值 <25 nM。它通过降低细胞中的 NAD+水平发挥细胞毒性作用，具有抗癌活性。

细胞实验: 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)

激酶实验: 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.

体外活性: 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]

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)


关键字: Nicotinamide phosphoribosyl transferase | CHS828 | NAMPT | inhibit | PBEF | Visfatin | Apoptosis | Inhibitor | GMX 1778 | Pre-B cell colony enhancing factor | GMX-1778 | CHS-828

相关产品: AZD5582 | AGN 192870 | AZ960 | OTS514 hydrochloride | Bendamustine hydrochloride | Alda-1 | STAT5-IN-2 | AES-350 | Glycochenodeoxycholic Acid | NM-3

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途