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Pathways Recommended: GPCR/G Protein
Results for "

Gαq

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111557
    YM-254890
    5+ Cited Publications

    P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM .
    YM-254890
  • HY-117037

    Apoptosis ERK Cardiovascular Disease Cancer
    FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .
    FR900359
  • HY-114994

    TSH Receptor Endocrinology
    MS437 is a potent TSH receptor (TSHR) stimulator with an EC50 value of 13x10 -8 M. MS437 shows potent activation of G, Gαq and Gα12 and up-regulation of thyroglobulin (Tg), sodium iodine symporter (NIS) and TSHR gene expressions .
    MS437
  • HY-148016

    Protease Activated Receptor (PAR) ERK Inflammation/Immunology
    I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research .
    I-287
  • HY-107916
    Thyrotropin
    1 Publications Verification

    TSH; Pretiron

    Others Metabolic Disease Endocrinology Cancer
    Thyrotropin is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism .
    Thyrotropin
  • HY-161317

    Trace Amine-associated Receptor (TAAR) Cancer
    Gαq/11 protein-IN-1 (compound F33) is an inhibitor of Gαq/11 protein with an IC50 value of 9.4 μM. Gαq/11 protein-IN-1 has antitumor activity .
    Gαq/11 protein-IN-1
  • HY-120816

    Others Cardiovascular Disease
    WU-07047, a simplified analog of YM-254890 (HY-111557), is a selective Gαq/11 inhibitor. WU-07047 can inhibit nucleotide exchange .
    WU-07047
  • HY-108554

    Protease Activated Receptor (PAR) Others
    Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
    Q94 hydrochloride
  • HY-103117

    5-HT Receptor Neurological Disease
    S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis=6.6 and 8.9 nM, respectively). It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor (Ki=5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s=38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s=38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.
    S 32212 hydrochloride

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