Aryl Hydrocarbon Receptor Antagonist

Aryl Hydrocarbon Receptor Antagonists (22):

Cat. No.	Product Name	Effect	Purity

HY-12028

PD98059	Antagonist	99.96%
PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC₅₀ of 2-7 µM) and MEK2 (IC₅₀ of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC₅₀ of 4 μM) and AHR transformation (IC₅₀ of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.

HY-12684

CH-223191	Antagonist	99.60%
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC₅₀ of 0.03 μM.

HY-112628

CAY10464	Antagonist
CAY10464 (AHR antagonist 7; compound 4j) is a selective and high-affinity aryl hydrocarbon receptor (AhR) antagonist with a K_i of 1.4 nM.

HY-15001

Stemregenin 1	Antagonist	99.87%
Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC₅₀ of 127 nM.

HY-135829

BAY 2416964	Antagonist	99.59%
BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC₅₀ of 341 nM. BAY 2416964 has the potential for solid tumors treatment.

HY-102023

GNF351	Antagonist	99.90%
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC₅₀ of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.

HY-125833

Alpha-Naphthoflavone	Antagonist	98.54%
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.

HY-111449

BAY-218	Antagonist	99.95%
BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC₅₀ of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.

HY-112629

PDM2	Antagonist	98.76%
PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an K_i of 1.2±0.4 nM.

HY-136220

AHR antagonist 5	Antagonist	98.05%
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC₅₀ of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.

HY-135831

AHR antagonist 2	Antagonist	99.91%
AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC₅₀s of 0.885 and 2.03 nM for human and mouse AhR.

HY-103220

6,2',4'-Trimethoxyflavone	Antagonist	98.09%
6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.

HY-N8572

3',4'-Dimethoxyflavone	Antagonist	98.76%
3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.

HY-118780

CHD-5	Antagonist	≥98.0%
CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist.

HY-136220A

AHR antagonist 5 hemimaleate	Antagonist
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC₅₀ of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).

HY-135830

AHR antagonist 4	Antagonist
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC₅₀ of 82.2 nM. AHR antagonist 4 has anti-cancer effects.

HY-N12537A

(2R,3S)-PD-1/PD-L1-IN-38	Antagonist
(2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8⁺T cells and inhibits the signal transduction of PD-1/PD-L1.

HY-15001A

Stemregenin 1 hydrochloride	Antagonist
Stemregenin 1 hydrochloride is a purine derivative that antagonizes aryl hydrocarbon receptor signaling in CD34+ cells. IC₅₀ The value is 127 nM. Stemregenin 1 hydrochloride can be used to expand the pluripotency of hematopoietic stem cells (HSC) in stem cell studies.

HY-155061

hCYP1B1-IN-1	Antagonist
hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC₅₀=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells.

HY-W338764

AHR agonist 3	Antagonist
AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research.

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