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Results for "

Gi activation

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

1

Biochemical Assay Reagents

9

Peptides

1

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1376A
    G-Protein antagonist peptide TFA

    		mAChR Adrenergic Receptor 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 .
    G-Protein antagonist peptide TFA
  • HY-P5358
    YFLLRNP

    		Protease Activated Receptor (PAR) 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))
    YFLLRNP
  • HY-156025
    HCAR2 agonist 1

    		Hydroxycarboxylic Acid Receptor (HCAR) Inflammation/Immunology
    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 .
    HCAR2 agonist 1
  • HY-164795A
    SBI-810 hydrochloride

    		Neurotensin Receptor Neurological Disease
    SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride 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 activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .
    SBI-810 hydrochloride
  • HY-P1376
    G-Protein antagonist peptide

    		mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
    G-Protein antagonist peptide
  • HY-175306
    GPR183 inverse agonist-1

    		EBI2/GPR183 Arrestin 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 .
    GPR183 inverse agonist-1
  • HY-P0258
    Mas7

    Mastoparan 7

    		 Apoptosis Cardiovascular Disease Neurological Disease
    Mas7 (Mastoparan 7), a structural analogue of mastoparan, is an activator of heterotrimeric Gi proteins and its downstream effectors.
    Mas7
  • HY-162669
    Mu opioid receptor antagonist 8

    		Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
    Mu opioid receptor antagonist 8
  • HY-164795
    SBI-810

    		Neurotensin Receptor Neurological Disease
    SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .
    SBI-810
  • HY-175231
    ST171

    		5-HT Receptor 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 .
    ST171
  • HY-117102
    ANI-7

    		Aryl Hydrocarbon Receptor Checkpoint Kinase (Chk) 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 .
    ANI-7
  • HY-157871
    TAK1-IN-5

    		MAP3K Cancer
    TAK1-IN-5 (Compound 26) is an inhibitor of the transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. TAK1-IN-5 can inhibit the growth of MPC-11 and H929 cells with a GI50 lower than 30 nM. TAK1-IN-5 can be used in the study of multiple myeloma .
    TAK1-IN-5
  • HY-P0172A
    ATI-2341 TFA
    2 Publications Verification

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    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) .
    ATI-2341 TFA
  • HY-P0172
    ATI-2341

    		CXCR Inflammation/Immunology Endocrinology Cancer
    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) .
    ATI-2341
  • HY-111385
    UNC9994 hydrochloride
    1 Publications Verification

    		 Dopamine Receptor 5-HT Receptor Arrestin Neurological Disease
    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 .
    UNC9994 hydrochloride
  • HY-170027
    LW1564

    		HIF/HIF Prolyl-Hydroxylase AMPK 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 .
    LW1564
  • HY-107024
    Osteogenic Growth Peptide (10-14)

    OGP(10-14); Historphin

    		 Src 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 .
    Osteogenic Growth Peptide (10-14)
  • HY-121140
    AZ1729

    		Free Fatty Acid Receptor Metabolic Disease
    AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .
    AZ1729
  • HY-119272
    EF24
    1 Publications Verification

    		 ERK Caspase NF-κB Apoptosis p38 MAPK Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    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 .
    EF24
  • HY-103211
    L748337
    1 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Metabolic Disease Cancer
    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 .
    L748337
  • HY-W745090
    Isomaltulose monohydrate

    		Formyl Peptide Receptor (FPR) Src ERK Akt p38 MAPK Others
    Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
    Isomaltulose monohydrate
  • HY-P1793A
    α-Casein (90-95) TFA

    		Opioid Receptor Biochemical Assay Reagents Neurological Disease Inflammation/Immunology Cancer
    α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA 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) TFA 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) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer .
    α-Casein (90-95) TFA
  • HY-P1793
    α-Casein (90-95)

    		Opioid Receptor Biochemical Assay Reagents Neurological Disease Inflammation/Immunology Cancer
    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 .
    α-Casein (90-95)

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