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

Cat.No. 产品名称 Information
GC33314 1,4-Chrysenequinone (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。
GC50422 10-Cl-BBQ Potent aryl hydrocarbon receptor (AhR) agonist; orally bioavailable
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。
GC35271 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.
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。
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。
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。
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。
GC60636 Benzyl butyl phthalate 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。
GC35553 Brevifolincarboxylic acid A phenol with anticancer and anti-inflammatory activities
GC47037 Carbidopa (hydrate) A dopamine decarboxylase inhibitor
GC18824 CAY10465 A resveratrol-based aryl hydrocarbon receptor agonist
GC16220 CH 223191
CH 223191是一种有效的芳烃受体（AhR）特异性拮抗剂，可抑制TCDD介导的AhR核转位和DNA结合，抑制TCDD诱导的荧光素酶活性，IC₅₀为0.03 μM。
GC67892 CHD-5 CHD-5 是一种有效的 AhR (芳香烃受体)拮抗剂。
GC45705 D-Kynurenine An antagonist of GPR109B
GN10706 Diosimin A citrus-derived flavonoid
GC36043 FICZ
FICZ (Formyl-indolo [3,2-b] carbazole), as an endogenous ligand for the aryl hydrocarbon receptor (AhR).
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.
GC16368 Indole-3-carbinol A natural phytochemical
GC12628 ITE An endogenous AhR agonist
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。
GC12040 L-Kynurenine An active metabolite of tryptophan
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。
GC30297 Mivotilate (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。
GC11817 PDM 2 A resveratrol-based aryl hydrocarbon receptor antagonist
GC10538 Pifithrin-α (PFTα) Pifithrin-α(PFT-α)是一种p53抑制剂,在神经科学中广泛用于阻断神经元凋亡细胞死亡, 也可以作为强效的芳烃受体(AhR)刺激物。.
GC44686 Prochloraz An imidazole antifungal
GC30646 Skatole(3-Methylindole) Skatole (3-methylindole, Scatole) is a mildly toxic white crystalline organic compound that occurs naturally in feces. It has a fairly broad bacteriostatic effect.
GC69908 Skatole-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。
GC17043 StemRegenin 1 (SR1) Antagonizes hematopoietic stem cell differentiation
GC31732 Tapinarof (WBI 1001) 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.