2. Protein Tyrosine Kinase/RTK Immunology/Inflammation NF-κB Anti-infection PI3K/Akt/mTOR Epigenetics Metabolic Enzyme/Protease Apoptosis
  3. VEGFR NOD-like Receptor (NLR) NF-κB Bacterial AMPK Acetyl-CoA Carboxylase Apoptosis Reactive Oxygen Species (ROS) HSV
  4. Isomangiferin

Isomangiferin is an orally active xanthone C-glucoside, and its chemical structure is similar to Mangiferin (HY-N0290). Isomangiferin is an effective VEGFR-2 kinase inhibitor, which can induces cell apoptosis, inhibit the growth, metastasis and angiogenesis of breast cancer. Isomangiferin exerts anti-inflammatory effects by inhibiting the HMGB1/NLRP3/NF-κB signaling pathway, thereby improving the renal function indicators of diabetic mice. Isomangiferin exhibits inhibitory effects on various bacteria and herpes simplex virus type 1 (HSV-1). Isomangiferin promotes the migration and osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) and reduces cell apoptosis and the production of ROS by activating the AMPK/ACC pathway, thereby facilitating fracture healing.

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Isomangiferin

Isomangiferin Chemical Structure

CAS No. : 24699-16-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of Isomangiferin:

Isomangiferin Related Antibodies

Top Publications Citing Use of Products

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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NLRP3 NLRP1 NOD1 NOD2

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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HSV-1 HSV-2 HSV

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Isomangiferin is an orally active xanthone C-glucoside, and its chemical structure is similar to Mangiferin (HY-N0290). Isomangiferin is an effective VEGFR-2 kinase inhibitor, which can induces cell apoptosis, inhibit the growth, metastasis and angiogenesis of breast cancer. Isomangiferin exerts anti-inflammatory effects by inhibiting the HMGB1/NLRP3/NF-κB signaling pathway, thereby improving the renal function indicators of diabetic mice. Isomangiferin exhibits inhibitory effects on various bacteria and herpes simplex virus type 1 (HSV-1). Isomangiferin promotes the migration and osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) and reduces cell apoptosis and the production of ROS by activating the AMPK/ACC pathway, thereby facilitating fracture healing[1][2][3][4][5].

In Vitro

Isomangiferin inhibits HSV-1 that exceeds Acyclovir (HY-17422), Idoxuridine (HY-B0307), and Cyclocytidine (HY-N0093) in log by 0.27-0.50 in log determination and exhibits the average plaque reduction rate of 69.5%[1].
Isomangiferin shows better antibacterial potential than Mangiferin against all the tested strain including B. subtilis, S. aureus, K. pneumoniae, S. Setubal, E. coli with MICs ≤ 250 μg/mL[2].
Isomangiferin shows poor cytotoxicity towards Brine shrimp nauplii with a LD50 of 768.92 mg/mL[2].
Isomangiferin (2.5-10 μM, 24 h) promotes osteogenic differentiation and migration of H2O2-treated bone marrow mesenchymal stem cells (BMSCs), reduces apoptosis and reactive oxygen species production, and activates the AMP-activated protein kinase/acetyl-CoA carboxylase (AMPK/ACC) pathway[3].
Isomangiferin (1 μM, 48 h) decreases the viability of breast cancer cells (MDA-MB-231, T47D, MCF7, SKBR3, 4T1) with IC50s of approximately 1 μM, , while the IC50 for the MCF-10A cells exceeded 100 μM[5].
Isomangiferin (1 μM, 5 days) inhibits microvessel sprouting and vascular tubulogenesis of endothelial cells[5].
Isomangiferin (0-5 μM, 1-36 h) inhibits migration and invasion and induces breast cancer cell apoptosis and impairs cell adhesion in MDA-MB-231 cells through VEGFR-2-mediated signaling pathway[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Isomangiferin Related Antibodies

Cell Viability Assay[3]

Cell Line: BMSCs stimulated with H2O2
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Dose-dependently restored cell viability.

Cell Migration Assay [3]

Cell Line: BMSCs stimulated with H2O2
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Restored the migration ability by 2.1 times at 10 μM.

Apoptosis Analysis[3]

Cell Line: BMSCs stimulated with H2O2
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Reduced the apoptosis rate to 11.3% at 10 μM.

ELISA Assay[3]

Cell Line: BMSCs stimulated with H2O2
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Restored the ALP activity to 90% of its normal level at 10 μM.
Reduced the level of ROS by 60% at 10 μM.

Western Blot Analysis[3]

Cell Line: BMSCs stimulated with H2O2
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Induced the upregulation of Runx2 and BMP2 expression.
Downregulated the pro-apoptotic protein Bax, upregulated the anti-apoptotic protein Bcl-2 and inhibited the activation of caspase-3.
Significantly increase the levels of p-AMPK and p-ACC (Ser79).

Cell Migration Assay [5]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, 2.5 and 5 μM
Incubation Time: 6 h
Result: Showed dose-dependent inhibition, and almost completely inhibited migration at 5 μM.

Cell Invasion Assay[5]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, 2.5 and 5 μM
Incubation Time: 8 to 10 h
Result: Showed dose-dependent inhibition, and almost completely inhibited invasion at 5 μM.

Apoptosis Analysis[5]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, 2.5 and 5 μM
Incubation Time: 36 h
Result: Increased the apoptosis rate from 7.15% to 13.06% at a concentration of 5 μM.

Western Blot Analysis[5]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, 2.5 μM
Incubation Time: 24 h
Result: Activated caspase-3 and PARP cleavage.
In Vivo

Isomangiferin (10-20 mg/kg, p.o., once daily for 12 weeks) provides protection against renal injury via inhibiting HMGB1/NLRP3/ NF-κB signaling in a diabetic mouse model[4].
Isomangiferin (10 mg/kg, i.p., once daily for a month) inhibits breast cancer growth and blocks the VEGFR-2 pathway in the xenograft model[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Type 2 diabetes mellitus (T2DM) model established in mice (C57BL/KsJ db/db mice, male) and male db/m mice[4]
Dosage: 10 and 20 mg/kg
Administration: Oral administration (p.o.), once daily for 12 weeks
Result: Reduced UA and Cr levels in Db/Db mice.
Reduced serum insulin levels and improved lipid profiles in Db/Db mice.
Attenuated kidney damage.
Reduced inflammatory cytokine levels in serum and the kidney.
Inhibited HMGB1/NACHT leucine-rich repeat- and PYD-containing 3 (NLRP3)/NF-κB pathway in Db/Db mice.
Animal Model: MDA-MB-231 induced xenograft model established in five-week-old male BALB/c nude mice[5]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for a month
Result: Significantly reduced the volume and weight of the tumor.
Significantly reduced the expression of p-VEGFR2 and CD31. Reduced the microvessel density (MVD) within the tumor tissue and the number of p-VEGFR2 positive cells.
Molecular Weight

422.34

Formula

C19H18O11
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

OC1=CC(O)=C2C(OC3=CC(O)=C(O)C=C3C2=O)=C1[C@@H]([C@@H]([C@@H](O)[C@@H]4O)O)O[C@@H]4CO
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (118.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3678 mL 11.8388 mL 23.6776 mL
5 mM 0.4736 mL 2.3678 mL 4.7355 mL
View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.92 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.92 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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.60%

SDS (393 KB)

COA (256 KB) LCMS (91 KB)

Handling Instructions (2659 KB)
References

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 (protect from light). 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 2.3678 mL 11.8388 mL 23.6776 mL 59.1940 mL
5 mM 0.4736 mL 2.3678 mL 4.7355 mL 11.8388 mL
10 mM 0.2368 mL 1.1839 mL 2.3678 mL 5.9194 mL
15 mM 0.1579 mL 0.7893 mL 1.5785 mL 3.9463 mL
20 mM 0.1184 mL 0.5919 mL 1.1839 mL 2.9597 mL
25 mM 0.0947 mL 0.4736 mL 0.9471 mL 2.3678 mL
30 mM 0.0789 mL 0.3946 mL 0.7893 mL 1.9731 mL
40 mM 0.0592 mL 0.2960 mL 0.5919 mL 1.4799 mL
50 mM 0.0474 mL 0.2368 mL 0.4736 mL 1.1839 mL
60 mM 0.0395 mL 0.1973 mL 0.3946 mL 0.9866 mL
80 mM 0.0296 mL 0.1480 mL 0.2960 mL 0.7399 mL
100 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.5919 mL
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Isomangiferin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Isomangiferin24699-16-9VEGFRNOD-like Receptor (NLR)NF-κBBacterialAMPKAcetyl-CoA CarboxylaseApoptosisReactive Oxygen Species (ROS)HSVVascular endothelial growth factor receptorNuclear factor-κBNuclear factor-kappaBAMP-activated protein kinaseACC, Acetyl Coenzyme A Carboxylase Herpes simplex virusDryopteris ramoseAntibacterialMangiferinXanthoneC-glycosidesCytotoxicBMSCsOsteogenic differentiationAMPK/ACC pathwayAngiogenesis inhibitorsBreast neoplasmsInhibitorinhibitorinhibit

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