CAS NO: | 555-55-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
Cas No. | 555-55-5 |
别名 | 6-[(1E)-2-(3,4-二羟基苯基)乙烯基]-4-羟基-2H-吡喃-2-酮 |
化学名 | 6-[(1E)-2-(3,4-dihydroxyphenyl)ethenyl]-4-hydroxy-2H-pyran-2-one |
Canonical SMILES | OC1=CC(/C=C/C(O2)=CC(O)=CC2=O)=CC=C1O |
分子式 | C13H10O5 |
分子量 | 0 |
溶解度 | ≤10mg/ml in DMSO |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 2 μM Hispidin is a protein kinase Cβ inhibitor. Protein Kinase C (PKC), a serine/threonine kinase, is activated by signal transduction pathways producing DAG from phosphatidylinositol diphosphate and phosphatidylcholine via the action of various activated phospholipases. Protein kinase Cβ (PKCβ) plays a critical role in the initiation of colon carcinogenesis in a preclinical mouse model by promoting proliferation and increased β-catenin accumulation. In vitro: In previous study hispidin was found to reduce cell viability in both mouse and human colon cancer cells, and the apoptotic cell morphological changes were also observed. These results showed accumulation of the sub-G1 cell population and increase in early apoptosis dose-dependently. Moreover, hispidin could induce apoptosis via up-regulation of both intrinsic and extrinsic apoptotic pathways. Although the molecular mechanism underlying hispidin-induced apoptosis was known to involve the generation of ROS, however hispidin was not able to display any apoptosis in the pre-treatment with N-acetyl-L-cysteine, a ROS scavenger [1]. In vivo: Previous animal study found that the treatment with PKC-activating agent phorbol-12-myristate-13-acetate could attenuate exendin-4-induced relaxations and reduced GLP-1R expression in Wistar-Kyoto rat arteries, which were reversed by hispidin [2]. Clinical trial: Up to now, hispidin is still in the preclinical development stage. References: |