京尼平 T2210

Product Introduction
Bioactivity


英文名: Genipin

描述: Genipin ((+)-Genipin) 是衍生自黄栀果实的天然交联剂，可抑制细胞中的 UCP2 (解偶联蛋白 2)。它有蛋白质调节、抗肿瘤、抗炎症、免疫抑制、抗血栓形成和对海马神经元保护的多种生物活性，可研究 2 型糖尿病。

激酶实验: Briefly, the peptide substrate N-acetyl-Asp-Glu-Val-Asp-ρ-nitroanilide (Ac-DEVD-ρNA) is added to the cell lysates in assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM dithiothreitol, 1 mM EDTA, 10% glycerol) and incubated at 37°C. The cleavage of the substrate is monitored at 405 nm.

体外活性: Genipin stimulats glucose uptake in a time- and dose-dependent manner. The maximal effect is achieved at 2?h with a concentration of 10?μM. In myotubes, genipin promotes glucose transporter 4 (GLUT4) translocation to the cell surface, which increases the phosphorylation of insulin receptor substrate-1 (IRS-1), AKT, and GSK3β. Meanwhile, genipin increases ATP levels, closed KATP channels, and then increases the concentration of calcium in the cytoplasm in C2C12 myotubes. Genipin-stimulated glucose uptake could be blocked by both the PI3-K inhibitor wortmannin and calcium chelator EGTA. Moreover, genipin increases the level of reactive oxygen species and ATP in C2C12 myotubes[1]. Genipin increases mitochondrial membrane potential, which then increases ATP levels and closes KATP channels, thereby stimulating insulin secretion in pancreatic β-cells. Genipin activates glucose-excited POMC neurons[2]. Cytochrome c content increases significantly in the cytosol of genipin-treated FaO cells. Activation of caspase-3 and caspase-7 is ultimately responsible for genipin-induced apoptotic process in hepatoma cells. ROS level notably increases in Hep3B cells treated with 200 μM genipin[3].

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

溶解度: Ethanol : 45 mg/mL (198.91 mM)
H2O : 1 mg/mL (4.42 mM)
DMSO : 45 mg/mL (198.91 mM)


关键字: UCP2 | immunosuppression | hippocampal | inhibit | anti-inflammation | DNMT1 | Autophagy | Inhibitor | reagent | proteins | Genipin | crosslinking | diabetes | antithrombosis | type-2 | antitumor

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相关库: Anti-Tumor Natural Product Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Human Endogenous Metabolite Compound Library Plus | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Natural Product Library for HTS | Miao medicine Compound Library | NO PAINS Compound Library | Natural Product 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