gq

GQ-16 is a partial agonist of PPARγ with a Ki of 160 nM. GQ-16 reduces adipogenic actions and promotes insulin Sensitization without weight gain.

GPLGIAGQ acetate is a MMP2-cleavable polypeptide. GPLGIAGQ acetate can be used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy.

Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes through phosphoinositide turnover. Ganglioside GQ1b mixture contains ganglioside GQ1b molecular species with C18:1 and C20:1 sphingoid backbones.

VSPPLTLGQLLS, also known as peptide P3, is a small peptide that serves as an inhibitor of FGFR3, effectively suppressing FGFR3 phosphorylation. It hinders 9-cisRA-induced tracheal lymphangiogenesis and impedes lymphatic endothelial cell (LEC) activities, including proliferation, migration, and tubule formation [1] [2].

VSPPLTLGQLLS TFA, a small peptide FGFR3 inhibitor also known as peptide P3, effectively inhibits FGFR3 phosphorylation. It also prevents 9-cisRA-induced tracheal lymphangiogenesis and impedes lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation [1] [2].

FLGFVGQALNALLGKL-NH2, an antimicrobial peptide derived from frogs, exhibits activity against Staphylococcus aureus ATCC 29213 with a minimum inhibitory concentration (MIC) of 32 μM [1].

GQN-B37-E is an effective selective binder and inhibitor of MCL-1. It binds to the BH3-binding domain of MCL-1. GQN-B37-E demonstrates binding affinity for MCL-1 within the sub-micromolar range (Ki= 0.6 μM), yet shows negligible binding to BCL-2 or BCL-XL.

NH2-QGGYTMHQDQEGDTDAGLK-COOH is a synthetic peptide chain featuring a primary amine group (NH2) attached to lysine and a carboxyl group (COOH) attached to glutamine.

GPLGIAGQ, a MMP2-cleavable polypeptide, functions as a stimulus-sensitive linker in liposomal and micellar nanocarriers for MMP2-triggered tumor targeting.

GPLGIAGQ TFA, is an MMP2-cleaved polypeptide that is used as a stimulus-sensitive connector in both liposomes and micelle nanoceroses for targeted therapy of tumors triggered by MMP2.

MGQTNDGAYRDPTDNN sodium is an antigenic and surface-exposed peptide from CotH3. CotH3 mediates fungal invasion of host cells during mucormycosis.

TRV120056 acetate is a Gq-biased agonist with 10-fold greater molecular efficiency on AT1R-Gq fusion proteins than AT1R-βarr2 fusion proteins.

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

GPR40 FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40 FFAR1) agonist and allosteric modulator.

Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.

SBI-810 is a functional selective β-arrestin-biased allosteric modulator of the neurotensin receptor 1 (NTSR1). In the presence of the endogenous ligand neurotensin (NT), SBI-810 regulates NTSR1 signaling through a G protein-specific mechanism. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, allowing NTSR1 to activate GoA and G12.

ECPLA is an LSD analog and a potent 5-HT2A agonist (EC50 of 14.6 nM), capable of stimulating Gq-mediated calcium flux. It exhibits high affinity for most serotonin receptors, α2-adrenergic receptors, and D2-like dopamine receptors.

SBI-810 hydrochloride is a functional selective allosteric modulator of the β-arrestin-biased neurotensin receptor 1 (NTSR1). It modulates NTSR1-G protein signaling in a G protein-specific manner in the presence of the endogenous ligand neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced Gq activation, partially antagonizes NT-induced Gi1 activation, while allowing activation of GoA and G12 by NTSR1.

EP-3945 is an agonist of Mas-related G protein-coupled receptors (MRGPR), exhibiting greater potency than the small molecule agonist β-Alanine targeting MRGPRD. MRGPRs play a crucial role in inflammatory itch and pain perception. These receptors interact with Gq (MRGPRX2, MRGPRX4, and MRGPRX1 are coupled with Gq; MRGPRX2 and MRGPRD couple with Gi), with EP-3945 having an EC50 value of 211.6 nM for Gq.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM) that shows efficacy in alleviating antipsychotic-like phenotypes and cognitive deficits in an MK-801-induced psychosis model in mice. It is applicable for research related to schizophrenia.

FR900359, a non-ribosomal cyclic peptide derived from the soil bacterium Chromobacterium oxysporum, is a macrocyclic Gq protein inhibitor that inhibits melanoma cell proliferation and can be used in studies of asthma, inflammation, and cancer.

FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999

TRV120055, a Gq-biased agonist, demonstrates a 10-fold higher molecular efficacy when tested against the AT1R-Gq fusion protein in comparison to the AT1R-βarr2 fusion protein.

TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.