タピナロフ
Based on 15 publication(s) in Google Scholar
Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.95%
- CAS 番号: 79338-84-4
- 分子式: C17H18O2
- 分子量:254.32
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保管条件:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Tapinarof
More- Redox Biol. 2021 Oct:46:102110. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424985122. [Abstract]
- EMBO J. 2026 Jan;45(1):261-277. [Abstract]
- Cell Chem Biol. 2026 Jan 15;33(1):91-101.e12. [Abstract]
- Cell Death Discov. 2026 Jan 9;12(1):16. [Abstract]
- Antioxidants (Basel). 2024 Jun 17;13(6):732. [Abstract]
- JCI Insight. 2021 Mar 8;6(5):e145185. [Abstract]
- J Invest Dermatol. 2023 Oct;143(10):1964-1972.e4. [Abstract]
- Int J Mol Sci. 2024 Jul 19;25(14):7910. [Abstract]
- Cell Oncol (Dordr). 2025 Dec 23;49(1):3. [Abstract]
- J Mol Cell Cardiol. 2025 Oct 21:209:104-118. [Abstract]
- Res Microbiol. 2023 Sep-Oct;174(7):104081. [Abstract]
- Exp Dermatol. 2024 Jan;33(1):e14862. [Abstract]
- Immun Inflamm Dis. 2023 Jun;11(6):e903. [Abstract]
- Clemson University. 2025.
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
生物活性
EC50: 13 nM (AhR)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CD4+ve Th | IC50 |
5.2 μM
Compound: Tapi
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Induction of apoptosis in human CD4+ve Th cells
Induction of apoptosis in human CD4+ve Th cells
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[PMID: 35123295] |
Tapinarof activates the AhR pathway through direct binding. Tapinarof dose-dependently induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) (EC50=0.16 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 79338-84-4
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性状 Solid
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分子量 254.32
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分子式 C17H18O2
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Color White to light yellow
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SMILES
OC1=C(C(C)C)C(O)=CC(/C=C/C2=CC=CC=C2)=C1
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別名
Tapinarof; WBI-1001; Benvitimod; GSK2894512
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (15)
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Journal Impact Factor
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Most Recent
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Redox Biol
Inhibition of 6-formylindolo[3,2-b]carbazole metabolism sensitizes keratinocytes to UVA-induced apoptosis: Implications for vemurafenib-induced phototoxicity. [Abstract]2021 Oct:46:102110. PMID: 34418602
Tapinarof purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Oct:46:102110. [Abstract]
CYP1A1 enzyme activity measurement in HaCaT cells and NHEKs treated for 24 h with 100 nM Tapinarof (n = 3).
Tapinarof purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Oct:46:102110. [Abstract]
CYP1A1 enzyme activity measurement in HaCaT cells and NHEKs treated for 24 h with 100 nM Tapinarof (n = 3).
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Proc Natl Acad Sci U S A
CRISPR screens and quantitative proteomics reveal remodeling of the aryl hydrocarbon receptor-driven proteome through PARP7 activity. [Abstract]2025 Jun 17;122(24):e2424985122. PMID: 40493189
Tapinarof purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424985122. [Abstract]
Quantitative proteomics (TMT 18-plex) volcano plots showing significantly upregulated (red) and downregulated (blue) proteins in HCC44 cells treated with 1 μM Tapinarof (24 h).
Tapinarof purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424985122. [Abstract]
Western blotting analysis of AHR and SOCS3 levels in HCC44 cells treated with 1 µM RBN2397 with or without 1 µM CH223191 and 1 µM Tapinarof (24 h).
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EMBO J
Ubiquitin pathway blockade reveals endogenous ADP-ribosylation marking PARP7 and AHR for degradation. [Abstract]2026 Jan;45(1):261-277. PMID: 41326691
Tapinarof purchased from MedChemExpress. Usage Cited in: EMBO J. 2026 Jan;45(1):261-277. [Abstract]
HCC44 cells were pre-treated with DMSO, 1 µM Tapinarof and PARP inhibitors (PARP1/2 (1 µM Olaparib), PARP7 (100 nM RBN2397), PARP14 (200 nM RBN012759), TNKS (1 µM AZ6102)) for 20 h followed by an additional 4 h of 1 µM TAK243 or 10 µM MG132 treatment.
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Cell Chem Biol
Identification of aryl hydrocarbon receptor as a functional target that enhances astrocytic ApoE secretion. [Abstract]2026 Jan 15;33(1):91-101.e12. PMID: 41483807 -
Cell Death Discov
ALDH3A1-dependent Nrf2/HO-1/GPX4 pathway supports AHR as a promising therapeutic target for ferroptosis and promotes imperatorin-mediated lung protection. [Abstract]2026 Jan 9;12(1):16. PMID: 41513604 -
Antioxidants (Basel)
Induction of Semaphorin 3A by Resveratrol and Pinostilbene via Activation of the AHR-NRF2 Axis in Human Keratinocytes. [Abstract]2024 Jun 17;13(6):732. PMID: 38929171 -
JCI Insight
2021 Mar 8;6(5):e145185. PMID: 33497363 -
J Invest Dermatol
Ligand-activation of the aryl hydrocarbon receptor up-regulates epidermal UDP-glucose ceramide glucosyltransferase and glucosylceramides. [Abstract]2023 Oct;143(10):1964-1972.e4. PMID: 37004877 -
Int J Mol Sci
Difamilast, a Topical Phosphodiesterase 4 Inhibitor, Produces Soluble ST2 via the AHR-NRF2 Axis in Human Keratinocytes. [Abstract]2024 Jul 19;25(14):7910. PMID: 39063153 -
Cell Oncol (Dordr)
PARP7 and aryl hydrocarbon receptor differentially regulate mammary cancer cell proliferation and STING-induced type I interferon signalling. [Abstract]2025 Dec 23;49(1):3. PMID: 41432900 -
J Mol Cell Cardiol
Beneficial effects of aryl hydrocarbon receptor activation on post-infarction myocardial metabolism, inflammation and fibrosis: implications from multi-omics. [Abstract]2025 Oct 21:209:104-118. PMID: 41130496 -
Res Microbiol
2023 Sep-Oct;174(7):104081. PMID: 37196776 -
Exp Dermatol
2024 Jan;33(1):e14862. PMID: 37350230 -
Immun Inflamm Dis
AhR agonist tapinarof ameliorates lupus autoimmunity by suppressing Tfh cell differentiation via regulation of the JAK2-STAT3 signaling pathway. [Abstract]2023 Jun;11(6):e903. PMID: 37382269 -
溶剤 & 溶解度
Ethanol : ≥ 100 mg/mL (393.21 mM)
DMSO : 100 mg/mL (393.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (9.83 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 (9.83 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.
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. * In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
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.
プロトコル
HaCaT cells (10,000 cells/well) are cultured in 96-well Greiner μCLEAR plates in 100 μL DMEM with HEPES, Glutamax and 10% fetal bovine serum to confluence. Media is replaced with 100 μL media containing 0.2% heat-inactivated, charcoal-stripped fetal bovine serum and incubated overnight. Titrating concentrations of Tapinarof (10-8 μM ,10-6 μM, 10-4 μM, 0.01 μM, and 1 μM) are added for 30 minutes followed by washing and fixing in ice-cold methanol:acetone (50:50). Samples are blocked with 3% BSA for 1 hour, and then washed again in phosphate buffered saline with 0.1% Tween-20. Next, cells are stained with 50 μL of 1:50 dilution anti-AhR antibody in 3% BSA, followed by 50 μL secondary antibody (1:500 dilution chicken anti-rabbit AlexaFluor488 and 1:2,000 dilution Hoechst 33342) in 3% BSA/phosphate buffered saline. Images are acquired on InCell 2000 and/or Opera. Image analysis is performed using InCell Analyzer Workstation and/or Columbus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 3.9321 mL | 19.6603 mL | 39.3205 mL | 98.3013 mL |
| 5 mM | 0.7864 mL | 3.9321 mL | 7.8641 mL | 19.6603 mL | |
| 10 mM | 0.3932 mL | 1.9660 mL | 3.9321 mL | 9.8301 mL | |
| 15 mM | 0.2621 mL | 1.3107 mL | 2.6214 mL | 6.5534 mL | |
| 20 mM | 0.1966 mL | 0.9830 mL | 1.9660 mL | 4.9151 mL | |
| 25 mM | 0.1573 mL | 0.7864 mL | 1.5728 mL | 3.9321 mL | |
| 30 mM | 0.1311 mL | 0.6553 mL | 1.3107 mL | 3.2767 mL | |
| 40 mM | 0.0983 mL | 0.4915 mL | 0.9830 mL | 2.4575 mL | |
| 50 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9660 mL | |
| 60 mM | 0.0655 mL | 0.3277 mL | 0.6553 mL | 1.6384 mL | |
| 80 mM | 0.0492 mL | 0.2458 mL | 0.4915 mL | 1.2288 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9830 mL |
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