Hispidin |
| カタログ番号GC15018 |
PKC 阻害剤であり、メシマコブからのフェノール化合物であるヒスピジンは、強力な抗酸化、抗がん、抗糖尿病、および抗認知症特性を有することが示されています 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 555-55-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 555-55-5 | SDF | |
| Chemical Name | 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 | ||
| Formula | C13H10O5 | M.Wt | 0 |
| 溶解度 | ≤10mg/ml in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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