Cat. No.: HY-109044

Tapinarof

(Synonyms: WBI-1001; Benvitimod; GSK2894512)

15 Cited Publications

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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.

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Pureté: 99.95%
CAS No.: 79338-84-4
Formule: C₁₇H₁₈O₂
Masse moléculaire:254.32

Stockage:

4°C, protect from light

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

Tapinarof Chemical Structure

CAS No.: 79338-84-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (15)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC₅₀ of 13 nM. Tapinarof resolves skin inflammation in mice^[1].

IC₅₀ & Target

EC50: 13 nM (AhR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CD4+ve Th	IC₅₀	5.2 μM Compound: Tapi	Induction of apoptosis in human CD4+ve Th cells Induction of apoptosis in human CD4+ve Th cells	[PMID: 35123295]

In Vitro

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.

In Vivo

Tapinarof acts through AhR to reduce inflammation in IMQ-treated mice. AhR-sufficient mice on a C57Bl/6 background exhibit a reduced clinical score after treatment with Tapinarof or 6-formylindolo(3,2-b)carbazole (FICZ). In contrast, AhR KO mice do not respond to the anti-inflammatory effects of Tapinarof. FICZ is used as a comparator in these studies and yields similar results, with dramatically reduced inflammatory responses in wild-type, but not AhR KO mice^[1].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 79338-84-4
Appearance Solid
Masse moléculaire 254.32
Formule C₁₇H₁₈O₂
Color White to light yellow
SMILES

OC1=C(C(C)C)C(O)=CC(/C=C/C2=CC=CC=C2)=C1
Synonyms

WBI-1001; Benvitimod; GSK2894512
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

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).
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).
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.
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

Particulate matter causes skin barrier dysfunction. [Abstract]

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

The AcrAB efflux pump confers self-resistance to stilbenes in Photorhabdus laumondii. [Abstract]

2023 Sep-Oct;174(7):104081. PMID: 37196776
Exp Dermatol

The opposite effect of tapinarof between IMQ and IL-23 induced psoriasis mouse models. [Abstract]

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
Clemson University

2025.

Solvant et solubilité

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.9321 mL

19.6603 mL

39.3205 mL

5 mM

0.7864 mL

3.9321 mL

7.8641 mL

10 mM

0.3932 mL

1.9660 mL

3.9321 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.83 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocole

Cell Assay^[1]

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.

Animal Administration^[1]

Mice^[1]
Female BALB/c mice (BALB/cByJRj) are used. Studies are performed using 100 µL of Tapinarof (1%) or FICZ (0.01%, at the limit of solubility) in 60% ethanol: 40% water^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Smith SH, et al. Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J Invest Dermatol. 2017 Oct;137(10):2110-2119. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Tapinarof

15 Cited Publications

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Tapinarof

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Publications Citing Use of MedChemExpress (MCE) Tapinarof

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tapinarof

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Osteogenesis Compound Library

Off-patent Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tapinarof

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tapinarof Related Classifications

HY-109044 Related Classifications