Tapinarof (Synonyms: WBI-1001; Benvitimod; GSK2894512)

Name: Tapinarof
Brand: MedChemExpress
SKU: HY-109044
Rating: 5.0 (15 reviews)

Cat. No.: HY-109044 Purity: 99.95%: Data Sheet
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Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC₅₀ of 13 nM. Tapinarof resolves skin inflammation in mice.

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

CAS No. : 79338-84-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Tapinarof:

Tapinarof-d₅ Get quote
(E/Z)-Tapinarof Get quote
Tapinarof (Standard) Get quote

15 Publications Citing Use of MCE Tapinarof

Bio/Physico-chemical Assay

: 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).

: 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.

: Tapinarof purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Oct:46:102110.; 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.; CYP1A1 enzyme activity measurement in HaCaT cells and NHEKs treated for 24 h with 100 nM Tapinarof (n = 3).

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Biological Activity
Protocol
Purity & Documentation
References
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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.

Clinical Trial

Molecular Weight

254.32

Formula

C₁₇H₁₈O₂

CAS No.

79338-84-4

Appearance

Solid

Color

White to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
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 (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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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, 1 year; -20°C, 6 months (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: 99.95%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (247 KB) HNMR (243 KB) RP-HPLC (255 KB) MS (238 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

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

Tapinarof Related Classifications

Inflammation/Immunology

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:

Tapinarof79338-84-4WBI-1001 Benvitimod GSK2894512WBI1001WBI 1001GSK2894512GSK 2894512GSK-2894512Aryl Hydrocarbon ReceptorAhRInhibitorinhibitorinhibit

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Tapinarof (Synonyms: WBI-1001; Benvitimod; GSK2894512)

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Other Forms of Tapinarof:

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15 Publications Citing Use of MCE Tapinarof

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Complete Stock Solution Preparation Table

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