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You are here:Home-Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-Aryl hydrocarbon Receptor (AhR)

Request The Product List ofAryl hydrocarbon Receptor (AhR) Aryl hydrocarbon Receptor (AhR)

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.

Cat. No. Product Name CAS No. Information
GY04399

CH-223191

301326-22-7

CH-223191 is a potent, specific antagonist of AhR (aryl hydrocarbon receptor), potently inhibits TCDD-induced AhR-dependent transcription with IC50 of 0.03 uM; shows more inhibitory potency and no agonist-like effect, compared with flavone, resveratrol, and α-naphthoflavone, as well as estrogenic potency; inhibits TCDD-AhR binding and TCDD-induced nuclear translocation and DNA binding of AhR, prevents the expression of cytochrome P450 enzymes, target genes of the AhR; potently prevents TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice

GY10036

CAY 10465

688348-33-6

CAY10465 is an analog of resveratrol acting as a potent and selective aryl hydrocarbon receptor agonist, with a Ki of 0.2 nM. CAY10465 is inactive as a ligand for the estrogen receptor even at 100 µM.

GY10035

PDM-2

688348-25-6

PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.

GY06596

FICZ

172922-91-7

FICZ is a high affinity aryl hydrocarbon receptor (AhR) agonist with Kd of 70 pM; induces transient expression of CYP1A1 in vitro, and potentiates NK cell IFN-γ production and cytolytic activity; enhances NK cell control of tumors in an NK cell- and AhR-dependent manner in vivo; an endogenous AhR ligand.

GY06594

TCDD

1746-01-6

TCDD is a potent AHR (aryl hydrocarbon receptor) agonist that induces degradation of AhR by the ubiquitin-proteasome pathway; suppresses the transcription of PEPCK and decreases Sirtuin 1 activation of PGC1α; also blocks cNK development and supports group 3 innate lymphoid cell (ILC3) differentiation.

GY03262

ITE

448906-42-1

ITE is a endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro; activates the murine AhR in vivo, but does not induce toxicity; induces the differentiation of stem-like cancer cells and reduces their tumorigenic potential in both subcutaneous and orthotopic xenograft tumour models.

GY10023

BAY-2335218

2162982-11-6

BAY-2335218 is an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2017202816A1, example 23, has an IC50 of 39.9 nM in human cell line.

GY06526

5F 203

260443-89-8

5F 203 is a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway; causes MCF-7 sensitive cells to arrest in G(1) and S phase, and induces DNA adduct formation, in contrast to AhR-deficient AH(R100) variant MCF-7 cells, induces CYP1A1 and CYP1B1 transcription; L-lysylamide prodrug Phortress (NSC 710305) demonstrats antitumor activity in vivo.

GY06518

Phortress

328087-38-3

The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway; causes MCF-7 sensitive cells to arrest in G(1) and S phase, and induces DNA adduct formation, in contrast to AhR-deficient AH(R100) variant MCF-7 cells, induces CYP1A1 and CYP1B1 transcription; demonstrats antitumor activity in vivo.

GY06487

NK150460

709640-62-0

NK150460 is a potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway; inhibits growth of not only most ER-positive, but also some ER-negative breast cancer cell lines, while never inhibiting growth of non-breast cancer cell lines; inhibits 17β-estradiol (E2)-dependent transcription without affecting binding of E2 to ER; does not induce histone H2AX phosphorylation or p53 expression, is a a novel AhR agonist dependent on AhR/ARNT and cytochrome P450 CYP1A1.

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