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
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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
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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.