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Home >> Signaling Pathways >> Immunology/Inflammation >> Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor(芳烃受体)

Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1.

Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.

Products for  Aryl Hydrocarbon Receptor

  1. Cat.No. 产品名称 Information
  2. GC33314 1,4-Chrysenequinone (Chrysene-1,4-dione)

    1,4-屈醌,Chrysene-1,4-dione

     1,4-Chrysenequinone (Chrysene-1,4-dione) 是一种多环芳香族醌，可作为芳烃受体 (AhR) 的激活剂。
  3. GC50422 10-Cl-BBQ Potent aryl hydrocarbon receptor (AhR) agonist; orally bioavailable
  4. GC68631 AhR agonist 2 AhR agonist 2 (Compound 12a) 是一种有效的芳烃受体 (AhR) 激动剂，EC50 为 0.03 nM。AhR agonist 2 诱导 AhR 的快速核富集，触发下游基因的转录并促进皮肤屏障修复。AhR agonist 2 具有研究银屑病的潜力。
  5. GC35271 AHR antagonist 1

    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 ligands.
  6. GC39669 AHR antagonist 2 AHR antagonist 2 是一种有效的芳香烃受体 (AHR) 拮抗剂，对人和小鼠的 IC50 值分别为 0.885，2.03 nM，详情请参见专利 WO2019101641A1，example 1。
  7. GC64275 AHR antagonist 5 AHR antagonist 5 是有效的，具有口服活性的芳香烃受体 (AHR) 拮抗剂，IC50 为 < 0.5 μM。AHR antagonist 5 联合检测点抑制剂 anti-PD-1 对肿瘤生长有抑制作用，详细信息请参见专利 WO2018195397，example 39。
  8. GC64208 AHR antagonist 5 free base AHR antagonist 5 free base 是一种选择性的、具有口服活性的芳烃受体 (AHR) 抑制剂。AHR antagonist 5 free base 有效阻止 AHR 从细胞质转移到细胞核。AHR antagonist 5 free base 对 AHR 的选择性高于其他受体、转运蛋白和激酶，并具有抗癌作用。
  9. GC39284 ANI-7 ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长，并有选择地抑制 MCF-7 乳腺癌细胞的生长，GI50 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶，并在敏感的乳腺癌细胞系中诱导 DNA 损伤，检查点激酶 (Chk2) 激活，S 期细胞周期停滞和细胞死亡。
  10. GC60636 Benzyl butyl phthalate

    邻苯二甲酸丁苄酯

     Benzylbutylphthalate是邻苯二甲酸酯(PAEs)的一员，通过上调Zeb1的表达，可引起血管瘤(HA)细胞的迁移和侵袭。Benzylbutylphthalate激活乳腺癌细胞中的芳香烃受体(AhR)，刺激SPHK1/S1P/S1PR3信号传导，促进转移性乳腺癌干细胞(BCSCs)的形成。
  11. GC35553 Brevifolincarboxylic acid

    短叶苏木酚酸

     A phenol with anticancer and anti-inflammatory activities
  12. GC47037 Carbidopa (hydrate)

    卡比多巴单水合物,(S)-(-)-Carbidopa monohydrate

     A dopamine decarboxylase inhibitor
  13. GC18824 CAY10465 A resveratrol-based aryl hydrocarbon receptor agonist
  14. GC16220 CH 223191

    1-甲基-N-[2-METHYL-4-[2-(2-甲苯基)二氮烯基]苯基-1H-吡唑-5-甲酰胺

     CH 223191是一种有效且特异性的芳烃受体（AhR）拮抗剂，可抑制TCDD介导的AhR核转位和DNA结合，并抑制TCDD诱导的荧光素酶活性，IC50为0.03 μM。
  15. GC67892 CHD-5 CHD-5 是一种有效的 AhR (芳香烃受体)拮抗剂。
  16. GC45705 D-Kynurenine

    犬尿氨酸

     An antagonist of GPR109B
  17. GN10706 Diosimin

    地奥司明

     A citrus-derived flavonoid
  18. GC36043 FICZ

    6-甲酰基吲哚并[3,2-B]咔唑,6-Formylindolo[3,2-b]carbazole

     FICZ（甲酰吲哚 咔唑）作为芳基烃受体 (AhR) 的内源性配体，可以发挥多效性作用，包括防止炎症、纤维化和氧化应激。
  19. GC34597 GNF351 GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 interacts directly with the AHR ligand binding pocket and competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM.
  20. GC16368 Indole-3-carbinol

    3-吲哚甲醇; I3C; 3-Indolemethanol

     A natural phytochemical
  21. GC12628 ITE An endogenous AhR agonist
  22. GC69347 KYN-101 KYN-101 是一种有效的、选择性的和具有口服活性的 AHR 抑制剂。KYN-101 降低 CYP1A1 mRNA 表达。KYN-101 具有抗癌活性。
  23. GC12040 L-Kynurenine

    L-犬尿氨酸

     An active metabolite of tryptophan
  24. GC70236 L-Kynurenine-13C10 sulfate hemihydrate L-Kynurenine-13C10 sulfate hemihydrate是13C标记的l -犬尿氨酸硫酸盐。
  25. GC64898 L-Kynurenine-d4-1 L-Kynurenine-d4-1 是 L-Kynurenine 氘代物。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。
  26. GC30297 Mivotilate (YH439)

    YH439

     Mivotilate (YH439) 是一种无毒、有效的芳烃受体 (AhR) 激活剂，可作为保肝剂。
  27. GC11817 PDM 2 A resveratrol-based aryl hydrocarbon receptor antagonist
  28. GC10538 Pifithrin-α (PFTα)

    2-(2-亚氨基-4,5,6,7-四氢苯并噻唑-3-基)-1-P-甲苯基乙酮氢溴酸盐,Pifithrin hydrobromide; PFTα hydrobromide

     Pifithrin-α是一种p53抑制剂。
  29. GC44686 Prochloraz

    咪鲜胺; BTS 40542

    An imidazole antifungal
  30. GC30646 Skatole(3-Methylindole)

    粪臭素; 3-Methylindole; 3-Methyl-1H-indole

     Skatole (3-methylindole, Scatole) is a mildly toxic white crystalline organic compound that occurs naturally in feces. It has a fairly broad bacteriostatic effect.
  31. GC69908 Skatole-d3

    3-Methylindole-d3; 3-Methyl-1H-indole-d3

     Skatole-d3 是 Skatole 的氘代物。Skatole 是肠道菌群产生的物质，通过激活芳基烃受体 (aryl hydrocarbon receptors) 和 p38 调节肠上皮细胞功能。
  32. GC17043 StemRegenin 1 (SR1)

    SR1

     Antagonizes hematopoietic stem cell differentiation
  33. GC31732 Tapinarof (WBI 1001)

    苯烯莫德; WBI-1001; Benvitimod; GSK2894512

     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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