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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Xanthohumol, a naturally occuring prenylated chalcone compound isolated from hops (the female inflorescences of Humulus lupulus), is an inhibitor of COX-1 and COX-2 enzymatic activity and shows chemopreventive effects as well as anti-cancer and anti-angiogenic activities. It binds to the N domain of VCP, suppressing function and impairing autophagosome maturation. It inhibits growth of a wide variety of human cancer cell lines by inhibiting proliferation and inducing apoptosis. Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.
ln Vitro |
ADP-induced blood platelet aggregation is markedly inhibited by xanthohumol, which also dramatically lowers fibrinogen receptor expression (the activated form of GPIIbIIIa) on the surface of platelets[1]. In control myocytes and in cells exposed to Ca2+ overload brought on by: (1) exposure to low K+ solutions; (2) periods of high frequency electrical stimulation; (3) exposures to isoproterenol; or (4) caffeine, xanthohumol (5-50 nM) decreases the frequency of spontaneously occurring Ca2+ sparks and Ca2+ waves. Without inhibiting ICa, xanthohumol (50–100 nM) lowers the rate of relaxation of electrically or caffeine-triggered Ca2+ transients; however, this action is negligible and isoproterenol reverses it at physiological temperatures. Additionally, xanthohumol reduces the SR's rate of recirculation and Ca2+ content[2]. When Xanthohumol is applied to endothelial cells, AMPK phosphorylation and activity rise. It has been confirmed by functional investigations employing biochemical methods that AMPK mediates the anti-angiogenic effect of xanthohumol. Xanthohumol activates AMPK through the action of CAMMKβ, not LKB1. By lowering eNOS phosphorylation, Xanthohumol-induced AMPK activation lowers nitric oxide (NO) levels in endothelial cells, according to an analysis of the downstream pathways. Lastly, Xanthohumol's anti-angiogenic action inactivates the AKT pathway apart from AMPK, indicating that these two signaling pathways operate independently of one another[3]. The formation of intracellular ROS contributes to the glioma cell death caused by xanthohumol. Glioma cell death is largely mediated by xanthohumol's suppression of the IGFBP2/AKT/Bcl2 pathway via miR-204-3p targeting[4].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Luzak B, et al. Xanthohumol from hop cones (Humulus lupulus L.) prevents ADP-induced platelet reactivity. Arch Physiol Biochem. 2016 Nov 18:1-7
[2]. Arnaiz-Cot JJ, et al. Xanthohumol modulates calcium signaling in rat ventricular myocytes: Possible Antiarrhythmic properties. J Pharmacol Exp Ther. 2016 Nov 4. pii: jpet.116.236588 [3]. Gallo C, et al. Hop derived flavonoid xanthohumol inhibits endothelial cell functions via AMPK activation. Oncotarget. 2016 Aug 1 [4]. Chen PH, et al. The miR-204-3p-targeted IGFBP2 pathway is involved in xanthohumol-induced glioma cell apoptotic death. Neuropharmacology. 2016 Nov;110(Pt A):362-75. [5]. Inokoshi J, et al. Expression of two human acyl-CoA:diacylglycerol acyltransferase isozymes in yeast and selectivity of microbial inhibitors toward the isozymes. J Antibiot (Tokyo). 2009;62(1):51-54. [6]. Buckwold VE, et al. Antiviral activity of hop constituents against a series of DNA and RNA viruses. Antiviral Res. 2004 Jan;61(1):57-62 |
Molecular Formula |
C21H22O5
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Molecular Weight |
354.4
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CAS # |
6754-58-1
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SMILES |
O(C([H])([H])[H])C1C([H])=C(C(=C(C=1C(/C(/[H])=C(\[H])/C1C([H])=C([H])C(=C([H])C=1[H])O[H])=O)O[H])C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])O[H]
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | |
5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | |
10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.