Aryl Hydrocarbon Receptor (AhR or AHR) is a cytoplasmic receptor and transcription factor that belongs to the family of basic helix-loop-helix transcription factors. The AhR is activated or inhibited by various types of exogenous and endogenous ligands. AhR is an important factor in immunity and tissue homeostasis, and structurally diverse compounds from the environment, diet, microbiome, and host metabolism can induce AhR activity, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD).
Endogenous ligands include indigoids, heme metabolites, eicosanoids, tryptophan derivatives, and equilenin. Exogenous ligands include polycyclic aromatic hydrocarbons, polychlorinated biphenyls, natural compounds, and small molecule compounds. The different structures and properties of AhR ligands mean that when they combine with AhR they have distinct biological effects.
Unliganded AHR is sequestered in the cytoplasm by chaperone proteins including Hsp90, AHR-interacting protein (AIP), and p23. Upon ligand binding, AHR translocates to the nucleus and heterodimerizes with ARNT. The AHR-ARNT complex regulates transcription by binding with high affinity to specific DNA sequences termed aryl hydrocarbon response elements located in the regulatory regions of target genes including CYP1A1, CYP1B1, and TIPARP.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PC15345 | 5-fluoro 203 | 260443-89-8 | AhR信号传导活化剂,A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway. |
PC14883 | 6,2',4'-Trimethoxyflavone | 720675-74-1 | 芳基烃受体拮抗剂 |
PC14882 | CH 223191 | 301326-22-7 | AhR拮抗剂,CH-223191是有效且特异性的芳烃受体(AhR) 拮抗剂。 CH-223191阻断TCDD与AhR的结合,IC50 为0.03 µM。 |
PC14886 | DiMNF | 14756-24-2 | AHR调节剂 |
PC14888 | ITE | 448906-42-1 | AhR激动剂,ITE 是一种有效的内源性芳香烃受体 (AhR) 激动剂,能够直接与 AHR 结合,Ki 值为 3 nM。ITE 具有免疫抑制作用。 |
PC14885 | L-Kynurenine. | 2922-83-0 | 芳烃受体(AhR)的内源性活化剂,L-Kynurenine是L-色氨酸的代谢物。它是一种芳香烃受体 (aryl hydrocarbon receptor) 激动剂。 |
PC14884 | MeBIO | 667463-95-8 | CDK/Cyclin/GSK-3/p25/AhR激动剂,MeBIO is a negative control analog of BIO, and an aryl hydrocarbon receptor (AhR) agonist. It causes redistribution of AhR to the nucleus. |
PC15387 | PDM 11 | 1032508-03-4 | 有效的选择性芳基烃受体(AhR)拮抗剂,PDM11 是抗氧化剂白藜芦醇的衍生物。PDM11 对辐射分解产生的羟基自由基引发的亚油酸胶束氧化没有明显的保护作用。PDM11 在白藜芦醇活性测定中不活跃。 |
PC15386 | PDM 2 | 688348-25-6 | 有效的选择性芳基烃受体(AhR)拮抗剂,PDM2 是一种选择性的高亲和力芳烃受体 (AhR) 拮抗剂,Ki 为 1.2±0.4 nM。 |
PC14887 | Phortress | 328087-38-3 | 抗肿瘤剂5F 203的前药,The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway. |
PC15333 | Pyocyanin | 85-66-5 | 芳烃受体活化剂 |
PC15323 | StemRegenin 1 (hydrochloride) | 芳烃受体信号传导拮抗剂 |