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Pathways Recommended:	GPCR/G Protein

Results for "

Gαq

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Angiotensin Receptor (3) Apoptosis (4) Bacterial (1) Biochemical Assay Reagents (1) Calcium Channel (1) CXCR (1) Drug Derivative (1) Endogenous Metabolite (1) ERK (4) GPR119 (1) Liposome (1) Neurotensin Receptor (1) P2Y Receptor (3) PKC (1) Protease Activated Receptor (PAR) (2) Trace Amine-associated Receptor (TAAR) (1) TSH Receptor (2) YAP (2)
By Research Areas:	Cancer (6) Cardiovascular Disease (7) Endocrinology (2) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (2)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	Phospholipids (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111557

YM-254890 15+ 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 .

HY-130463

POPG sodium salt PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)	Liposome Biochemical Assay Reagents Neurotensin Receptor	Neurological Disease
POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ₁γ₁ for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .

HY-107916

Thyrotropin 1 Publications Verification TSH; Pretiron	TSH Receptor PKC Apoptosis	Metabolic Disease Inflammation/Immunology Endocrinology Cancer
Thyrotropin (TSH, Pretiron) 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 prevents Apoptosis. 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 .

HY-117037

FR900359 4 Publications Verification	Apoptosis ERK	Cardiovascular Disease Cancer
FR900359 is a depsipeptide selective inhibitor of Gα_q/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 Ovalbumin, low endotoxin (HY-W250978A)-induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .

HY-148016

I-287	Protease Activated Receptor (PAR) ERK	Inflammation/Immunology
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gα_q and Gα_12/13 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 .

HY-P3136

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-114994

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

HY-P3136A

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-P3910

[Val4] Angiotensin III	Angiotensin Receptor	Cardiovascular Disease
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gα_q and βarr2 response, with pEC₅₀ values of 8.31 and 8.44, respectively .

HY-120816

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

HY-161317

Gαq/11 protein-IN-1	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 .

HY-108554

Q94 hydrochloride	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 .

HY-103117

S 32212 hydrochloride	5-HT Receptor	Neurological Disease
S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC₅₀=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.

HY-179165

Gαq/11 protein-IN-2	P2Y Receptor Apoptosis YAP	Cancer
Gαq/11 protein-IN-2 (Compound 9g) is a Gαq/11 protein inhibitor, with an IC₅₀ of 11.3 μM. Gαq/11 protein-IN-2 induces Apoptosis, increases p-YAP. Gαq/11 protein-IN-2 has anticancer activity against uveal melanoma .

HY-182405

GQ127	Apoptosis YAP ERK	Cancer
GQ127 is an orally active Gαq/11 inhibitor with an IC₅₀ of 22.6 μM. GQ127 binds directly to Gαq/11 protein and inhibits its activity. GQ127 induces Apoptosis, suppresses viability, migration and invasion of uveal melanoma cells. GQ127 increases the phosphorylation level of YAP and decreases the phosphorylation level of ERK. GQ127 inhibits the growth of uveal melanoma xenografts in mouse models. GQ127 can be used for research related to uveal melanoma .

HY-N17826

YM-254891	Drug Derivative Bacterial P2Y Receptor Endogenous Metabolite	Cardiovascular Disease
YM-254891 is a YM-254890 (HY-111557) analogue and Gαq/11 inhibitor. YM-254891 can be isolated from the fermentation broth of Chromobacterium sp. QS3666. YM-254891 inhibits ADP-induced platelet aggregation .

HY-115643

AZ13581837	GPR119	Metabolic Disease
AZ13581837 is a GPR120 agonist with oral effectiveness, human EC₅₀ values of 5.2 nM, and mouse EC₅₀ of 4.3 nM. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes .

HY-182774

YU241279	CXCR	Cancer
YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma .

Cat. No.	Product Name	Target	Research Area

HY-P3136

TRV055 TRV120055	Angiotensin Receptor ERK	Cardiovascular Disease
TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-P3136A

TRV055 hydrochloride TRV120055 hydrochloride	Angiotensin Receptor	Cardiovascular Disease
TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses ^[1]

HY-P3910

[Val4] Angiotensin III	Angiotensin Receptor	Cardiovascular Disease
[Val4] Angiotensin III is an angiotension III peptide. [Val4] Angiotensin III is a potent full agonist of Gα_q and βarr2 response, with pEC₅₀ values of 8.31 and 8.44, respectively .

YM-254890 15+ Cited Publications	Cardiovascular Disease Natural Products Microorganisms Classification of Application Fields Disease Research Fields Source Classification	P2Y Receptor
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 .

FR900359 4 Publications Verification	Structural Classification Ardisia crenata Sims Ketones, Aldehydes, Acids Plants Myrsinaceae Source Classification	Apoptosis ERK
FR900359 is a depsipeptide selective inhibitor of Gα_q/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 Ovalbumin, low endotoxin (HY-W250978A)-induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .

YM-254891	Structural Classification Natural Products Microorganisms Source Classification	Drug Derivative Bacterial P2Y Receptor Endogenous Metabolite
YM-254891 is a YM-254890 (HY-111557) analogue and Gαq/11 inhibitor. YM-254891 can be isolated from the fermentation broth of Chromobacterium sp. QS3666. YM-254891 inhibits ADP-induced platelet aggregation .

Cat. No.	Product Name		Classification

HY-115643

AZ13581837		Alkynes
AZ13581837 is a GPR120 agonist with oral effectiveness, human EC₅₀ values of 5.2 nM, and mouse EC₅₀ of 4.3 nM. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes .

Cat. No.	Product Name		Classification

HY-130463

POPG sodium salt PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)		Phospholipids
POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ₁γ₁ for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .

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Gαq

Inhibitors & Agonists

Peptides

NaturalProducts

Click Chemistry

Oligonucleotides

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