Isoxanthohumol
Based on 4 publication(s) in Google Scholar
Isoxanthohumol is an orally active flavonoid compound. Isoxanthohumol has biological activities such as anti-tumor, anti-inflammatory, antioxidant, antiviral, antifungal, and inhibition of adipogenesis. Isoxanthohumol can induce apoptosis, autophagy, and migration of tumor cells. Isoxanthohumol is active against viruses such as HSV, BVDV, CMV, and Rhino. Isoxanthohumol can be used for the research of tumors, metabolic, and inflammatory diseases.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 521-48-2
- Formula: C21H22O5
- Molecular Weight:354.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Isoxanthohumol (Standard)Standard of Isoxanthohumol -
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AurapteneMMP Inhibitor; PPARα Agonists -
HY-N0306
Hederasaponin BAntiviral Agent -
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20(R)-Ginsenoside Rh2Anti-tumor/Anti-viral/Anti-inflammatory Agent -
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Hederasaponin B (Standard)Enterovirus Inhibitor -
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Auraptene (Standard)MMP Inhibitor; PPARα Agonists -
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20(R)-Ginsenoside Rh2 (Standard)Standard of 20(R)-Ginsenoside Rh2
Publications Citing Use of MedChemExpress (MCE) Isoxanthohumol
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Customer Validation & Images
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WB
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RT-PCR
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Cell Migration/Invasion Assay
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IF
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In Vivo Efficacy Study
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-29 | IC50 |
88.82 μM
Compound: 3
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Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
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[PMID: 23434138] |
| Ishikawa | IC50 |
24.9 μM
Compound: IX
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Cytotoxicity against human Ishikawa cells after 96 hrs by SRB assay
Cytotoxicity against human Ishikawa cells after 96 hrs by SRB assay
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[PMID: 28812892] |
| MCF7 | IC50 |
15.3 μM
Compound: IX
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 2 days by SRB assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 2 days by SRB assay
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[PMID: 33257172] |
| MCF7 | IC50 |
26.54 μM
Compound: 3
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Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay
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[PMID: 23434138] |
| MCF7 | IC50 |
4.69 μM
Compound: IX
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 4 days by SRB assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 4 days by SRB assay
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[PMID: 33257172] |
| PC-3 | IC50 |
71.32 μM
Compound: 3
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Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
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[PMID: 23434138] |
In Vitro
Isoxanthohumol (0-100 μM; 20 min-6 d) reduces the viability, induces apoptosis of mature 3T3-L1 adipocytes, and inhibits the differentiation of 3T3-L1 preadipocytes. The mechanisms are associated with ROS generation and mitochondrial dysfunction[1].
Isoxanthohumol (2.5-50 µg/mL) inhibits Botrytis cinerea, Fusarium graminearum, and Sclerotinia sclerotiorum with EC50 values of 4.32, 16.50, and 14.52 µg/mL, respectively[2].
Isoxanthohumol (1.6-100 μM; 0-7 d) suppresses the proliferation, adhesion, migration, invasion, and colony formation, induces apoptosis and autophagy, and downregulates the integrin signaling pathway in B16-F10 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Mature 3T3-L1 adipocytes
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Concentration:0, 25, 50, 75 and 100 μM
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Incubation Time:24 and 48 h
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Result:Inhibited the cell viability in a dose-dependent manner.
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Cell Line:B16-F10 cells
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Concentration:30 μM
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Incubation Time:0, 2, 6, 24 and 48 h
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Result:Inhibited the levels of integrin α-6、FAK、vinculin、Rho and α-SMA.
In Vivo
Isoxanthohumol (60 mg/kg; oral gavage; 8 days) shows ameliorative effects in a DSS (HY-116282C)-induced mouse colitis model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice treated B16-F10 cells[3]
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Dosage:20 mg/kg
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Administration:Oral administration; 18 days
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Result:Reduced the number and diameter of lung metastatic nodules.
Significantly decreased the expression of HMGB1 in lung metastatic cells, while enhanced the expression of S100 protein, and decreased the expression of the proliferation marker Ki-67, indicating the differentiation of metastatic cells to a less invasive phenotype.
Caused no significant toxicity.
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Animal Model:Male SPF C57BL/6 mice aged 6-8 weeks old treated DSS (HY-116282C)[4]
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Dosage:60 mg/kg
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Administration:Oral gavage; 8 days
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Result:Significantly attenuated DSS-induced colitis, evidenced by reduced DAI scores and histological improvements.
Suppressed pro-inflammatory Th17/Th1 cells, promoted anti-inflammatory Treg cells. Restored gut microbiota disorder, increased gut microbiota diversity.
Upregulated D-(+)-mannose and L-threonine, and regulated pyruvate metabolic pathway.
Chemical Information
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CAS No. 521-48-2
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Appearance Solid
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Molecular Weight 354.40
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Formula C21H22O5
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Color Off-white to light yellow
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SMILES
OC1=CC(OC)=C2C(CC(OC2=C1C/C=C(C)\C)C3=CC=C(C=C3)O)=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Phytother Res
Xanthohumol inhibits non-small cell lung cancer via directly targeting T-lymphokine-activated killer cell-originated protein kinase. [Abstract]2023 Jul;37(7):3057-3068. PMID: 36882184 -
Int J Mol Sci
Dual Targeting of HIF-1α and DLL4 by Isoxanthohumol Potentiates Immune Checkpoint Blockade. [Abstract]2026 Feb 5;27(3):1576. PMID: 41683994
Isoxanthohumol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2026 Feb 5;27(3):1576. [Abstract]
HEK293 cells were treated with STP (10 µM, positive control) or Isoxanthohumol (IXN) (10 µM) under hypoxic conditions for 24 h, and HIF-1α protein levels were determined by Western blot.
Isoxanthohumol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2026 Feb 5;27(3):1576. [Abstract]
HEK293 cells were treated with STP (10 µM) or Isoxanthohumol (IXN) (10 µM) under hypoxia for 24 h, and VEGFA mRNA expression was quantified by RT-qPCR.
Isoxanthohumol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2026 Feb 5;27(3):1576. [Abstract]
Wound healing assay: EA.hy926 monolayers were scratched, treated with STP (10 µM) or Isoxanthohumol (IXN) (10 µM) for 1 h, followed by VEGF-A (10 ng/mL) stimulation for 24 h. Representative images of wound closure.
Isoxanthohumol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2026 Feb 5;27(3):1576. [Abstract]
CD31 (green, blood vessels) expression was assessed by immunofluorescent assay treated with Isoxanthohumol (IXN) (2 mg/kg, i.p.).
Isoxanthohumol purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2026 Feb 5;27(3):1576. [Abstract]
Tumor volume was measured from day 7 post-injections throughout the treatment period treated with Isoxanthohumol (IXN) (2 mg/kg, i.p.).
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Vet Microbiol
The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]2026 May:316:110992. PMID: 41865607 -
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (141.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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3T3-L1 preadipocyte-to-adipocyte differentiation
3T3-L1 preadipocytes are induced to differentiate after growth arrest using adipogenic media containing insulin, dexamethasone, and IBMX; differentiation is assessed by lipid-droplet accumulation, triglyceride increase, Oil Red O staining, and adipocyte-marker induction such as PPARγ and C/EBPα.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
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Lipid Droplets: Oil Red O/Sudan Dye Lipid Staining
Lipid droplets are intracellular organelles with a neutral-lipid core that stores triacylglycerols and sterol esters, and Oil Red O or Sudan dyes detect these hydrophobic lipid deposits by partitioning into retained lipids in fresh or frozen specimens. Oil Red O stains neutral triglycerides and lipids in frozen tissue sections or air-dried cytologic preparations, while Sudan Black B has also been used as a histochemical fat stain for lipid-rich tissue structures.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Yang JY, et al. Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis. Apoptosis. 2007 Nov;12(11):1953-63. [Content Brief]
[2]. Yan YF, et al. The Antifungal Mechanism of Isoxanthohumol from Humulus lupulus Linn. Int J Mol Sci. 2021 Oct 7;22(19):10853. [Content Brief]
[3]. Krajnović T, et al. The hop-derived prenylflavonoid isoxanthohumol inhibits the formation of lung metastasis in B16-F10 murine melanoma model. Food Chem Toxicol. 2019 Jul;129:257-268. [Content Brief]
[4]. Yang YN, et al. Therapeutic effects and mechanisms of isoxanthohumol on DSS-induced colitis: regulating T cell development, restoring gut microbiota, and improving metabolic disorders. Inflammopharmacology. 2024 Jun;32(3):1983-1998. [Content Brief]
[5]. Żołnierczyk AK, et al. Isoxanthohumol--Biologically active hop flavonoid. Fitoterapia. 2015 Jun;103:71-82. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | 70.5418 mL |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | 14.1084 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL | 7.0542 mL | |
| 15 mM | 0.1881 mL | 0.9406 mL | 1.8811 mL | 4.7028 mL | |
| 20 mM | 0.1411 mL | 0.7054 mL | 1.4108 mL | 3.5271 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1287 mL | 2.8217 mL | |
| 30 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3514 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7635 mL | |
| 50 mM | 0.0564 mL | 0.2822 mL | 0.5643 mL | 1.4108 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1757 mL | |
| 80 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8818 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2822 mL | 0.7054 mL |
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