Tapinarof

For research use only.

Catalog No.S9700 Synonyms: GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505

Tapinarof Chemical Structure

CAS No. 79338-84-4

Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM.

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Biological Activity

Description Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM.
Targets
AhR [1]
(in immortalized keratinocytes)
apoptosis [1]
(in CD4+ T cells)
0.16 nM(EC50) 5.2 μM
In vitro

Tapinarof binds and activates AhR in multiple cell types, including cells of the target tissue –human skin. In addition, tapinarof moderates proinflammatory cytokine expression in stimulated peripheral blood CD4+ T cells and ex vivo human skin, and impacts barrier gene expression in primary human keratinocytes; both of these processes are likely to be downstream of AhR activation based on current evidence.[1]

In vivo

The anti-inflammatory properties of tapinarof derive from AhR agonism is conclusively demonstrated using the mouse model of imiquimod-induced psoriasiform skin lesions. Topical treatment of AhR-sufficient mice with tapinarof leads to compound-driven reductions in erythema, epidermal thickening and tissue cytokine levels. In contrast, tapinarof has no impact on imiquimod-induced skin inflammation in AhR-deficient mice.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: HaCaT cells
  • Concentrations: 0.01 pM - 1 μM
  • Incubation Time: 30 min
  • Method:

    HaCaT cells (10,000 cells/well) are cultured in 96-well plates in 100 μL DMEM with HEPES, Glutamax and 10% FBS to confluence. Media is replaced with 100 μl media containing 0.2% heat-inactivated, charcoal-stripped FBS and incubated overnight. Titrating concentrations of tapinarof 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, then washed again in PBS with 0.1% Tween-20. Next, cells are stained with 50μL of 1:50 dilution anti-AhR antibody in 3% BSA, followed by 50 μl secondary antibody in 3% BSA/PBS.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 51 mg/mL (200.53 mM)
Ethanol 51 mg/mL (200.53 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 254.32
Formula

C17H18O2

CAS No. 79338-84-4
Storage powder
in solvent
Synonyms GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04634695 Recruiting -- Pregnancy Malaria Obafemi Awolowo University|University of Copenhagen|LSHTM|European and Developing Countries Clinical Trials Partnership (EDCTP) August 10 2020 --
NCT04042103 Completed Drug: Tapinarof cream 1% Plaque Psoriasis Dermavant Sciences GmbH July 23 2019 Phase 2
NCT02637206 Completed Drug: GSK2894512 Cream|Drug: Vehicle Cream|Drug: Empty Patch Dermatitis Atopic GlaxoSmithKline October 27 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID