高车前素 TQ0201

Product Introduction
Bioactivity


英文名: Hispidulin

描述: Hispidulin 是存在于豚草中的一种黄酮，是Pim-1抑制剂，IC50值为2.71 μM。

细胞实验: HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 μM) for 24, 48 and 72 h. Following treatment, cells are further incubated with MTT reagents at 37°C for 4 h before DMSO is added, to dissolve formazan crystals, and absorbance is measured at 570 nm in a microplate reader [2].

动物实验: The tumor is established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40 mg/kg/day for 35 days. The body weight of tumor-bearing mice is recorded every week and tumor volume is calculated [2].

体外活性: Hispidulin在HepG2细胞中以剂量依赖和时间依赖的方式诱导细胞死亡。Hispidulin通过线粒体功能障碍诱导细胞凋亡，表现为Bcl-2/Bax比率下降、线粒体膜电位破坏以及细胞色素C释放增加和caspase-3激活[2]。

体内活性: Hispidulin治疗有效预防去卵巢引起的体重减轻，并减轻去卵巢引起的骨质流失。Hispidulin治疗还减少了去卵巢小鼠的小梁间隙[3]。在腹腔内给予大鼠Hispidulin（10或50mg/kg）30分钟后，再腹腔内注射海因酸（15mg/kg），可以延长发作潜伏期，降低发作评分。此外，Hispidulin显著减轻海因酸引起的海马神经元细胞死亡，这种保护效果伴随着海马中微胶质激活的抑制以及诸如白细胞介素-1β、白细胞介素-6和肿瘤坏死因子-α等促炎细胞因子产生的抑制[4]。

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

溶解度: H2O : Insoluble
DMSO : 60 mg/mL (199.82 mM)


关键字: Pim kinases | Hispidulin | Inhibitor | Pim | inhibit

相关产品: CX-6258 hydrochloride | HTH-01-091 | GDC-0339 | XL413 | FD1024 | TCS-PIM-1-4a | (Z)-SMI-4a | K00135 | Uzansertib phosphate | Pim1/AKK1-IN-1

相关库: Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Apoptosis Compound Library | Natural Product Library for HTS | Miao medicine Compound Library | Anti-Pancreatic Cancer Compound Library | Flavonoid Natural Product Library | Stem Cell Differentiation 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