1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR35

GPR35

G Protein-Coupled Receptor 35

GPR35 is an orphan G protein-coupled receptor (GPCR) that is highly expressed in the gastrointestinal (GI) tract, predominantly in colon epithelial cells (CEC). Kynurenic acid, a metabolite of L-tryptophan, has been proposed to be the endogenous ligand of GPR3535. Upon kynurenic acid-mediated GPR35 activation, β-arrestin 2 translocates to the cell membrane to mediate GPR35 internalization, resulting in receptor desensitization. Single nucleotide polymorphisms of GPR35 have linked this receptor to inflammatory bowel disease and primary sclerosing cholangitis, suggesting a role in gastrointestinal inflammation. In addition, in conjunction with previous findings that link agonism of GPR35 with significant reduction in nociceptive pain, GPR35 has emerged as a potential effector of regulation of mechanical sensitivity and analgesia of the Ret tyrosine kinase, and as a receptor involved in the transmission of anti-inflammatory effects of aspirin– potentially through affecting leukocyte rolling, adhesion and extravasation.

GPR35 Related Products (21):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100806
    Kynurenic acid
    Agonist 98.58%
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid
  • HY-W008613
    Pamoic acid
    Agonist 98.63%
    Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC50 of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties.
    Pamoic acid
  • HY-B1816
    Zaprinast
    Agonist 99.95%
    Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
    Zaprinast
  • HY-107537
    CID 2745687
    Agonist 98.07%
    CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM.
    CID 2745687
  • HY-107536
    ML 145
    ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.
    ML 145
  • HY-W008613R
    Pamoic acid (Standard)
    Agonist
    Pamoic acid (Standard) is the analytical standard of Pamoic acid. This product is intended for research and analytical applications. Pamoic acid (Embonic acid) is a potent GPR35 agonist with an EC50 of 79 nM. Pamoic acid exhibits neuroprotective and anti-inflammatory properties.
    Pamoic acid (Standard)
  • HY-169301
    Gpr35 modulator 1
    Modulator
    Gpr35 modulator 1 (compound 1-18) is a potent modulator of Gpr35, with the IC50 of ≤ 100 nM in HEK293 cells stably transfected with human GPR35.
    Gpr35 modulator 1
  • HY-169304
    Gpr35 modulator 3
    Modulator
    Gpr35 modulator 3 (Example 105) is a Gpr35 modulator with an IC50 < 1 μM. Gpr35 modulator 3 can be used in the study of proliferative, immune, and inflammatory.
    Gpr35 modulator 3
  • HY-100806S
    Kynurenic acid-d5
    Agonist 98.35%
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8[1][2].
    Kynurenic acid-d<sub>5</sub>
  • HY-107512
    Kynurenic acid sodium
    Agonist 99.79%
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
  • HY-W010907
    Pamoic acid disodium
    Agonist ≥98.0%
    Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.
    Pamoic acid disodium
  • HY-134801
    CID1231538
    99.74%
    CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR).
    CID1231538
  • HY-101033
    GPR35 agonist 1
    99.22%
    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good agentgability.
    GPR35 agonist 1
  • HY-149190
    GPR35 agonist 5
    Agonist 98.86%
    GPR35 agonist 5 (3,5-dinitro-bisphenol A; compound 6) is a weak GPR35 agonist. GPR35 agonist 5 arrests CHO-S cells at the G1/Gophase.
    GPR35 agonist 5
  • HY-15705
    GPR35 agonist 2
    Agonist 98.84%
    GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively.
    GPR35 agonist 2
  • HY-107538
    YE120
    Agonist 99.80%
    YE120 is a potent GPR35 agonist with an EC50 of 32.5 nM.
    YE120
  • HY-100806R
    Kynurenic acid (Standard)
    Agonist
    Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid (Standard)
  • HY-107539
    GPR35 agonist 4
    Agonist ≥99.0%
    GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC50 of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.
    GPR35 agonist 4
  • HY-101958
    Tyrphostin 25
    Agonist 99.00%
    Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and an EC50 of 5.3 µM.
    Tyrphostin 25
  • HY-131728
    GPR35 agonist 3
    Agonist 98.32%
    GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50value of 1.4 μM. GPR35 agonist 3 can be used for the research of various diseases, such as gastric cancer, type 2 diabetes, cardiovascular diseases, immune system and peripheral nervous system.
    GPR35 agonist 3