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Hispidin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hispidin图片
CAS NO:555-55-5
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Hispidin 是一种 PKC 抑制剂和桑黄中的一种酚类化合物,已被证明具有很强的抗氧化、抗癌、抗糖尿病和抗痴呆的特性。
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 SMILESOC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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:
[1] Lim JH, Lee YM, Park SR, Kim DH, Lim BO.  Anticancer activity of hispidin via reactive oxygen species-mediated apoptosis in colon cancer cells. Anticancer Res. 2014 Aug;34(8):4087-93.
[2] Liu L, Liu J, Gao Y, Ng CF, Yu X, Dou D, Huang Y.  Protein kinase Cβ mediates downregulated expression of glucagon-like peptide-1 receptor in hypertensive rat renal arteries. J Hypertens. 2015 Apr;33(4):784-90; discussion 790.