Home Metabolism AhR agonist - Apoptosis related activator Tapinarof For research use only.

Tapinarof

Synonyms: GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505

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.

Tapinarof Chemical Structure

Tapinarof Chemical Structure

CAS No. 79338-84-4

Purity & Quality Control

Batch: S970001 DMSO]51 mg/mL]false]Ethanol]51 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Tapinarof Related Products

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
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]
Cell Research 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.
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05979896 Recruiting
Malaria
Malaria Consortium
 July 28 2023 Phase 4
NCT05478954 Active not recruiting
Malaria
Malaria Consortium
 July 15 2022 Phase 4
NCT05471544 Active not recruiting
Malaria
Malaria Consortium
 July 18 2022 Phase 3
NCT05326659 Unknown status
Psoriasis
Peking University People''s Hospital|Zhonghao Pharmaceutical
 April 2022 Not Applicable
NCT05326672 Unknown status
Atopic Dermatitis
Peking University People''s Hospital|Zhonghao Pharmaceutical
 April 2022 Phase 3
NCT05172726 Recruiting
Plaque Psoriasis
Dermavant Sciences Inc.
 December 2 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 254.32 Formula

C17H18O2
CAS No. 79338-84-4 SDF --
Smiles CC(C)C1=C(O)C=C(\C=C\C2=CC=CC=C2)C=C1O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 51 mg/mL ( (200.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 51 mg/mL

Water : Insoluble


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