AHR antagonist 1

BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligand

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5mg

￥812.00

650.00

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10mg

￥1412.00

1130.00

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25mg

￥3162.00

2530.00

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50mg

￥5287.00

4230.00

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100mg

￥9175.00

7340.00

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200mg

￥0.00

0.00

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500mg

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0.00

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Background

Mechanistically, BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. In vitro, BAY-218 rescues TNFα production from kynurenic acid(KA)-suppressed LPS-treated primary human monocytes[1].

In vivo, BAY-218 enhances anti-tumoral immune responses and reduced tumor growth in the syngeneic mouse tumor models CT26 and B16-OVA. Furthermore, BAY-218 enhances therapeutic efficacy of an anti-PD-L1 antibody in the CT26 model[1].

[1] Ilona Gutcher, et al. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr 1288.