52 Results for "

Gi activation

" in MedChemExpress (MCE) Product Catalog:
Products (52)

52 Results for "Gi activation" in MCE Product Catalog:

4
4 Cited Publications
Cat. No.: HY-P0172
CAS No.: 1337878-62-2
Target:  

CXCR

ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
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4
4 Cited Publications
Cat. No.: HY-P0172A
Target:  

CXCR

ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
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3
3 Cited Publications
Cat. No.: HY-111385
CAS No.: 2108826-33-9
Purity:  98.83%
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
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2
2 Cited Publications
Cat. No.: HY-119272
CAS No.: 342808-40-6
Purity:  99.34%
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
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2
2 Cited Publications
Cat. No.: HY-103211
CAS No.: 244192-94-7
Purity:  ≥99.0%
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
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1
1 Cited Publications
Cat. No.: HY-W140439
CAS No.: 19420-56-5
Synonyms: 18:1 Lyso PC
Target:  

Endogenous Metabolite

Research Areas:  

Inflammation/Immunology

1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
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1
1 Cited Publications
Cat. No.: HY-107579
CAS No.: 72420-38-3
Purity:  99.25%
Synonyms: AY 25712
Target:  

GPR109A ERK

Acifran (AY 25712) is an orally active, full GPR109A and GPR109B agonist and hypolipidemic agent. Acifran reduces Forskolin (HY-15371)-induced cAMP elevation, triggers ERK1/ERK2 phosphorylation, and inhibits lipolysis in adipose tissue through Gi-coupled GPCR activation. Acifran is used for research on atherosclerosis, hyperlipidemia, and type 2 diabetes .
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1
1 Cited Publications
Cat. No.: HY-118830
CAS No.: 59894-07-4
Purity:  99.90%
Synonyms: DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2
13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2; 15-Oxo-13,14-dihydro-PGD2; 13,14-Dihydro-15-keto-PGD2) is a metabolite of Prostaglandin D2 (HY-101988) and acts as a CRTH2 agonist. 13,14-Dihydro-15-keto-prostaglandin D2 exhibits binding activity to CRTH2, induces cellular calcium signaling flux, and mediates eosinophilia in vivo. 13,14-Dihydro-15-keto-prostaglandin D2 activates the CRTH2 receptor, triggering Gi-dependent intracellular calcium mobilization and promoting the migration and recruitment of leukocytes from bone marrow to peripheral blood in vivo. 13,14-Dihydro-15-keto prostaglandin D2 is used in research on inflammation-related diseases, such as bronchial asthma .
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1
1 Cited Publications
Cat. No.: HY-P1376A
Research Areas:  

Endocrinology

G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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1
1 Cited Publications
Cat. No.: HY-P72428
Purity:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: VSIR; V-Set Immunoregulatory Receptor; C10orf54; SISP1; VISTA; B7-H5; PD-1H; Dies1; Gi24; B7H5; V-Type Immunoglobulin Domain-Containing Suppressor Of T-Cell activation; V-Set Domain-Containing Immunoregulatory Receptor; V-Domain Ig Suppressor Of T Cell Ac
Species:  
Mouse
Source:  
HEK293
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Cat. No.: HY-107024
CAS No.: 105250-85-9
Purity:  99.77%
Synonyms: OGP(10-14); Historphin
Target:  

Src

Research Areas:  

Others

Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor .
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Cat. No.: HY-117102
CAS No.: 931417-26-4
Purity:  98.13%
Research Areas:  

Cancer

ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
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Cat. No.: HY-P1793
CAS No.: 83471-50-5
α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer .
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Cat. No.: HY-156025
CAS No.: 1066676-21-8
Purity:  99.11%
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
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Cat. No.: HY-175231
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .
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Cat. No.: HY-170027
CAS No.: 2668337-39-9
Research Areas:  

Cancer

LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
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Cat. No.: HY-149933
CAS No.: 871978-21-1
AM841 is a cannabinoid superagonist and a covalent, irreversible full agonist of CB1. AM841 can activate peripheral CB1 receptors to reduce excitatory neurotransmission and GI smooth muscle contractility, and inhibit synaptic transmission. AM841 is peripherally restricted at low doses in mice, with extremely low brain penetration, potently inhibits gastrointestinal motility, and can reverse acute stress-induced hyperaccelerated gastrointestinal transit; at high doses, it can produce the classic tetrad of central cannabinoid phenotypes (analgesia, catalepsy, hypothermia, decreased spontaneous activity). AM841 can improve intestinal inflammation in mouse colitis models. AM841 induces transient stress-induced hyperthermia. AM841 can be used for research on gastrointestinal motility disorders and colitis .
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Cat. No.: HY-P0258
CAS No.: 145854-59-7
Synonyms: Mastoparan 7
Target:  

Apoptosis

Mas7 (Mastoparan 7), a structural analogue of mastoparan, is an activator of heterotrimeric Gi proteins and its downstream effectors.
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Cat. No.: HY-P5358
CAS No.: 149440-16-4
Research Areas:  

Others

YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
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Cat. No.: HY-175306
CAS No.: 2380033-51-0
Target:  

EBI2/GPR183 Arrestin

Research Areas:  

Inflammation/Immunology Cancer

GPR183 inverse agonist-1 (Compound 78) is a GPR183 inverse agonist. GPR183 inverse agonist-1 inhibits the GPR183-mediated Gi activation and β-arrestin2 recruitment, and blocks PBMC migration. GPR183 inverse agonist-1 can be used for inflammatory, autoimmune and neoplastic disorders research .
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