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Hispidin蛋白激酶Cβ抑制剂

Hispidin

产品编号:C3523
ApexBio 的所有产品仅用作科研,我们不为任何个人用途提供产品和服务
规格 单价 库存 订购数量
1mg ¥845.00 10-15 工作日发货
5mg ¥3,380.00 10-15 工作日发货

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Sample solution is provided at 25 µL, 10mM.

质量控制

质量控制和MSDS

批次:

化学结构

Hispidin

Hispidin Dilution Calculator

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Hispidin Molarity Calculator

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化学性质

CAS号 555-55-5 SDF Download SDF
化学名 6-[(1E)-2-(3,4-dihydroxyphenyl)ethenyl]-4-hydroxy-2H-pyran-2-one
SMILES OC1=CC(/C=C/C(O2)=CC(O)=CC2=O)=CC=C1O
分子式 C13H10O5 分子量 246.2
溶解度 ≤10mg/ml in DMSO 储存条件 Store at -20°C
物理性状 A crystalline solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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.