2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK STAT Wnt β-catenin
  4. Wilforine

Wilforine is an orally active JAK-STAT pathway inhibitor with immunomodulatory effects and the ability to inhibit osteoclast fusion. Wilforine disrupts lipid raft integrity, reprograms cholesterol and glycosphingolipid metabolic pathways, regulates NF-κB and the complement system, and modulates the expression of various interleukins. Wilforine also inhibits the Wnt11/β-catenin signaling pathway and suppresses the proliferation of fibroblast-like synoviocytes. Wilforine can serve as a quality and pharmacokinetic marker for Tripterygium glycoside tablets, and can be applied to research on related diseases such as rheumatoid arthritis, inflammatory osteolysis, and SAPHO syndrome.

For research use only. We do not sell to patients.

Wilforine

Wilforine Chemical Structure

CAS No. : 11088-09-8

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Other Forms of Wilforine:

Wilforine Related Antibodies

Top Publications Citing Use of Products

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

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Wnt1 Wnt3 Wnt5 Wnt7 Wnt11

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Wilforine is an orally active JAK-STAT pathway inhibitor with immunomodulatory effects and the ability to inhibit osteoclast fusion. Wilforine disrupts lipid raft integrity, reprograms cholesterol and glycosphingolipid metabolic pathways, regulates NF-κB and the complement system, and modulates the expression of various interleukins. Wilforine also inhibits the Wnt11/β-catenin signaling pathway and suppresses the proliferation of fibroblast-like synoviocytes. Wilforine can serve as a quality and pharmacokinetic marker for Tripterygium glycoside tablets, and can be applied to research on related diseases such as rheumatoid arthritis, inflammatory osteolysis, and SAPHO syndrome[1][2][3].

IC50 & Target[1]

Wnt11

 

In Vitro

Wilforine (100 μM; 6 days) inhibits osteoclast fusion in RAW264.7 cells by suppressing the JAK-STAT pathway, reducing expression of lipid raft scaffold proteins Stomatin and Flotillin-1, disrupting lipid raft integrity, and impairing localization and expression of fusion-related proteins CD9 and DC-STAMP[1].
Wilforine (200-400 nM) dose-dependently inhibits the proliferation of collagen-induced arthritis fibroblast-like synoviocytes (CIA FLS)[2].
Wilforine (30-300 μM; 20 h) induces significant cytotoxicity in human hepatoma HepG2 cells at concentrations of 30, 100, and 300 μM, with viability decreasing in a concentration-dependent manner[3].

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

Wilforine Related Antibodies

Cell Proliferation Assay[2]

Cell Line: Wnt11-overexpressing collagen-induced arthritis fibroblast-like synoviocytes (CIA FLS)
Concentration: 400 nM (wilforine treatment); optimal MOI (adenovirus infection)
Incubation Time: 36-48 h (adenovirus infection before wilforine treatment)
Result: Reduced relative CCK-8 detection value of CIA FLS from ~3.2 (untreated) to ~1.8 (wilforine-treated).
Reversed the inhibitory effect in Wnt11-overexpressing CIA FLS, with relative CCK-8 detection value increased to ~2.8.

Cell Cytotoxicity Assay[3]

Cell Line: human hepatoma HepG2 cells
Concentration: 30 μM; 100 μM; 300 μM
Incubation Time: 20 h
Result: Caused a significant reduction in HepG2 relative viability compared to the control group at 30 μM.
Caused highly significant reductions in HepG2 relative viability compared to the control group at 100 μM and 300 μM.
In Vivo

Wilforine (10-20 mg/kg; p.o.; daily; 28 days) dose-dependently alleviates inflammatory osteolysis in Pstpip2cmo mice[1].
Wilforine (40-56 μg/kg; p.o.; daily; from day 7 post-first immunization through day 35 post-first immunization) dose-dependently alleviates collagen-induced arthritis in rats, with significant reductions in arthritis scores, inflammatory cytokines, and pathological gene expression via inhibition of the Wnt11/β-catenin signaling pathway[2].
Wilforine (10-90 mg/kg; p.o.; daily; 21 days), administered as part of TGT suspension, dose-dependently reduces paw swelling in adjuvant arthritis rats and exhibits dose-dependent and time-dependent plasma AUC0-tn values, with significant toxicity (4 deaths) observed at the 90 mg/kg dose[3].

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

Animal Model: C57BL/6N Pstpip2cmo mice (both male and female, 6 weeks old, body weight 25 g)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; daily; 28 days
Result: Significantly reduced arthritis scores and paw thickness compared to the model group, with the 20 mg/kg dose showing superior efficacy.
Reduced bone destruction and clearer joint margins in treated mice, with the 20 mg/kg dose showing greater improvement.
Demonstrated dose-dependent reductions in cartilage erosion, synovial hyperplasia, inflammatory cell infiltration, cartilage matrix degradation, and periarticular fibrosis; the 20 mg/kg dose restored near-normal cartilage structure and tidemark clarity.
Significantly suppressed joint and paw expression of pro-inflammatory cytokines IL-1β and IL-6, and increased anti-inflammatory cytokine IL-10 expression compared to the model group (20 mg/kg dose).
Significantly downregulated joint expression of lipid raft scaffold proteins Stomatin and Flotillin-1, and osteoclast fusion-related proteins CD9 and DC-STAMPcompared to the model group (20 mg/kg dose).
Animal Model: Sprague-Dawley (SD) (male, 160-180 g, SPF grade, collagen-induced arthritis model)[2]
Dosage: 40 μg/kg; 48 μg/kg; 56 μg/kg
Administration: p.o.; daily; from day 7 post-first immunization through day 35 post-first immunization
Result: Dose-dependently reduced arthritis scores, hind paw swelling, and pain sensitivity (increased paw withdrawal threshold), and restored body weight.
Dose-dependently reduced serum levels of IL-1β, IL-6, and TNF-α.
Decreased mRNA levels of MMP3 and fibronectin in joint synovium.
Alleviated synovial hyperplasia, pannus formation, and bone/cartilage damage.
Dose-dependently reduced mRNA levels of Wnt11, CCND1, GSK-3β, and c-Myc in synovium.
Molecular Weight

867.85

Formula

C43H49NO18
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(OCC(C1OC(C)=O)(C(C(OC(C2=CC=CC=C2)=O)C3OC(C4C)=O)OC(C)=O)C(OC(C)(COC(C5=CC=CN=C5CC4)=O)C6C1OC(C)=O)(C3(O)C)C6OC(C)=O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (57.61 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 1.1523 mL 5.7614 mL 11.5227 mL
5 mM 0.2305 mL 1.1523 mL 2.3045 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. 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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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 (2.88 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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: 99.47%

SDS (392 KB)

COA (271 KB) HNMR (169 KB) CNMR (204 KB) RP-HPLC (203 KB) MS (143 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. 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 1.1523 mL 5.7614 mL 11.5227 mL 28.8068 mL
5 mM 0.2305 mL 1.1523 mL 2.3045 mL 5.7614 mL
10 mM 0.1152 mL 0.5761 mL 1.1523 mL 2.8807 mL
15 mM 0.0768 mL 0.3841 mL 0.7682 mL 1.9205 mL
20 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
25 mM 0.0461 mL 0.2305 mL 0.4609 mL 1.1523 mL
30 mM 0.0384 mL 0.1920 mL 0.3841 mL 0.9602 mL
40 mM 0.0288 mL 0.1440 mL 0.2881 mL 0.7202 mL
50 mM 0.0230 mL 0.1152 mL 0.2305 mL 0.5761 mL
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Wilforine 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:

Wilforine11088-09-8JAKSTATWntβ-cateninJanus kinaseBeta catenincollagen-induced arthritis fibroblast-like synoviocytesPstpip2cmo miceWnt11/β-catenin signalingJAK-STAT signaling pathwayinflammatory osteolysisHepG2 cellsfibroblast-like synovial cellsrheumatoid arthritis fibroblast-like synoviocytesRAW264.7 cellsNF-κBInhibitorinhibitorinhibit

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