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G-Protein

" in MedChemExpress (MCE) Product Catalog:

391

Inhibitors & Agonists

7

Screening Libraries

1

Biochemical Assay Reagents

88

Peptides

1

Inhibitory Antibodies

42

Natural
Products

111

Recombinant Proteins

33

Isotope-Labeled Compounds

35

Antibodies

1

Click Chemistry

19

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1376A

    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-P5985
    mSIRK
    1 Publications Verification

    ERK Others
    mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC50 of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .
    mSIRK
  • HY-137677B

    Guanosine 5'-[γ-thio]triphosphate tetralithium

    GLUT Others
    GTPγS (tetralithium) (Guanosine 5'-[γ-thio]triphosphate (tetralithium)) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .
    GTPγS tetralithium
  • HY-15565
    APD668
    2 Publications Verification

    GPR119 Cytochrome P450 Potassium Channel Metabolic Disease
    APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
    APD668
  • HY-10499
    PH-064
    2 Publications Verification

    BIM-46187

    Others Neurological Disease
    PH-064 (BIM-46187) is an inhibitor of heterotrimeric G-protein complex.
    PH-064
  • HY-70075
    CCG-63808
    2 Publications Verification

    RGS Protein Cancer
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
    CCG-63808
  • HY-P0195
    Bombesin
    1 Publications Verification

    Bombesin Receptor Neurological Disease Metabolic Disease
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors .
    Bombesin
  • HY-133021

    N-Acetyl-S-farnesyl-L-cysteine

    DNA Methyltransferase Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site .
    Arazine
  • HY-P1376

    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-10499A

    BIM-46187 tetrahydrochloride

    Endogenous Metabolite Neurological Disease
    PH-064 tetrahydrochloride is an inhibitor of heterotrimeric G-protein complex.
    PH-064 (tetra(hydrochloride))
  • HY-15565R

    GPR119 Cytochrome P450 Potassium Channel Metabolic Disease
    APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
    APD668 (Standard)
  • HY-B0412S1

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-d1
  • HY-19863A

    NLX-101 tosylate

    5-HT Receptor Neurological Disease
    F-15599 tosylate is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
    F-15599 tosylate
  • HY-19863
    F-15599
    2 Publications Verification

    NLX-101

    5-HT Receptor Neurological Disease
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
    F-15599
  • HY-P0216
    A 779
    10+ Cited Publications

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
    A 779
  • HY-149336

    Dopamine Receptor Neurological Disease
    D1R antagonist 1 (compound 12a) is a D1R antagonist, involved in G-protein- and β-arrestin-based signaling .
    D1R antagonist 1
  • HY-B0412S

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d2 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-d2
  • HY-B0412S2

    Isotope-Labeled Compounds Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d3 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-d3
  • HY-B0412S3

    Oestriol-13C3

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol- 13C3 is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
    Estriol-13C3
  • HY-123837

    Dopamine Receptor Neurological Disease
    MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling .
    MLS1082
  • HY-163917

    Opioid Receptor Neurological Disease
    SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .
    SalA-VS-08
  • HY-161106

    GPR84 Inflammation/Immunology Cancer
    OX04528 (compound 68) is a potent, G-protein biased, and orally active GPR84 agonist. OX04528 no cytotoxicity. OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM .
    OX04528
  • HY-P4414

    Orphan Receptor Neuropeptide B/W Receptor Neurological Disease
    (Des-Bromo)-Neuropeptide B (1-23) (human) is an orphan G-protein coupled receptor agonist with Kis of 1.2 nM and 341 nM for GPR7 (NPBW1) and GPR8 (NPBW2), respectively .
    (Des-Bromo)-Neuropeptide B (1-23) (human)
  • HY-174728

    mRNA Inflammation/Immunology
    Human CXCR1 mRNA encodes the human C-X-C motif chemokine receptor 1 (CXCR1) protein, a member of the G-protein-coupled receptor family. CXCR1 is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system.
    Human CXCR1 mRNA
  • HY-141495
    (Rac)-Razpipadon
    1 Publications Verification

    PW0464

    Dopamine Receptor Neurological Disease
    PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP) .
    (Rac)-Razpipadon
  • HY-175197

    Opioid Receptor Arrestin Neurological Disease
    MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research .
    MP1202
  • HY-160540

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MRGPRX2 modulator-1 (example 17) is a mas-related g-protein receptor x2 (MRGPRX2) modulator. MRGPRX2 modulator-1 can be used for the research of inflammation, pain and autoimmune disorders .
    MRGPRX2 modulator-1
  • HY-P1944A
    Apelin-13 TFA
    5+ Cited Publications

    Apelin Receptor (APJ) Cardiovascular Disease Metabolic Disease
    Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome .
    Apelin-13 TFA
  • HY-161107

    GPR84 Inflammation/Immunology
    OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .
    OX04529
  • HY-P2249

    Arrestin Apelin Receptor (APJ) Cardiovascular Disease
    ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
    ELA-21 (human)
  • HY-115768
    Compound 48/80
    1 Publications Verification

    Poly-p-methoxyphenethylmethylamine

    Phospholipase Neurological Disease Cancer
    Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
    Compound 48/80
  • HY-P1944
    Apelin-13
    5+ Cited Publications

    Apelin Receptor (APJ) Cardiovascular Disease Metabolic Disease
    Apelin-13 is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome .
    Apelin-13
  • HY-154954
    Ogremorphin
    1 Publications Verification

    OGM; GPR68-IN-1

    GPR68 Ferroptosis Inflammation/Immunology Cancer
    Ogremorphin (OGM) is a G protein coupled sensor GPR68 inhibitor with anti-inflammatory and anti-tumor activities. Ogremorphin can inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells .
    Ogremorphin
  • HY-162728

    Opioid Receptor Neurological Disease
    RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .
    RO-76
  • HY-149337

    Dopamine Receptor Neurological Disease
    D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
    D3R ligand 1
  • HY-175099

    Drug Intermediate Neurological Disease
    AB-ICA is a precursor of AB-FUBICA (HY-117403). AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity .
    AB-ICA
  • HY-163277

    Opioid Receptor Inflammation/Immunology
    PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
    PIPE-3297
  • HY-P5986

    ERK Others
    mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .
    mSIRK (L9A)
  • HY-122251

    RGS Protein Others Neurological Disease
    CCG-4986 is an RGS protein inhibitor. CCG-4986 inhibits protein activity by covalently modifying the Cys-132 site of RGS4. CCG-4986 can be used to study diseases related to dysregulated G protein-coupled receptor (GPCR) signaling, such as Parkinson's disease and opioid addiction .
    CCG-4986
  • HY-111216

    Melatonin Receptor Cancer
    CGP52608 is a selective agonist for the RZR/ROR receptor, known for its anti-tumor activity, and has almost no affinity for the cell surface G-protein coupled melatonin receptor. CGP52608 can inhibit the growth of mouse 16/C breast cancer cells. CGP52608 can induce the formation of vesicles in diatoms .
    CGP52608
  • HY-P5084

    Neuromedin U Receptor (NMUR) G protein-coupled Bile Acid Receptor 1 Neurological Disease
    Neuromedin S (human) is a neuropeptide that contains 33 amino acids. Neuromedin S (human)has been identified in the brain as an endogenous ligand for the orphan G-protein coupled receptor (GPCR) FM-4/TGR-1 and acts on the neuromedin U (NMU) receptor 2 (NMUR2) in the regulation of body weight homeostasis .
    Neuromedin S (human)
  • HY-137592

    ε-NAD

    Fluorescent Dye Others
    Nicotinamide 1,N6-ethenoadenine dinucleotide (ε-NAD) , a fluorescent analogue of NAD, is able to serve as a substrate for the bacterial toxincatalyzed G-ADP ribosylation of signal-transducing G-proteins. Nicotinamide 1,N6-ethenoadenine dinucleotide can be used as a fluorescent substrate for the studies of the ADP ribosylation reaction .
    Nicotinamide 1,N6-ethenoadenine dinucleotide
  • HY-145997

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders .
    MRGPRX4 modulator-1
  • HY-P1306

    GHSR Cardiovascular Disease Inflammation/Immunology
    Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
    Obestatin(rat)
  • HY-137592A

    ε-NAD sodium

    Others Others
    Nicotinamide 1,N6-ethenoadenine dinucleotide (ε-NAD) sodium, a fluorescent analogue of NAD, is able to serve as a substrate for the bacterial toxincatalyzed G-ADP ribosylation of signal-transducing G-proteins. Nicotinamide 1,N6-ethenoadenine dinucleotide sodium can be used as a fluorescent substrate for the studies of the ADP ribosylation reaction .
    Nicotinamide 1,N6-ethenoadenine dinucleotide sodium
  • HY-174787

    mRNA Cancer
    Human ACKR3 mRNA encodes the human atypical chemokine receptor 3 (ACKR3) protein, a member of the G-protein coupled receptor family. ACKR3 is a typical chemokine receptor that controls chemokine levels and localization via high-affinity chemokine binding that is uncoupled from classic ligand-driven signal transduction cascades, resulting instead in chemokine sequestration, degradation, or transcytosis.
    Human ACKR3 mRNA
  • HY-P1306A

    GHSR Cardiovascular Disease Inflammation/Immunology
    Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
    Obestatin(rat) TFA
  • HY-174727

    mRNA Inflammation/Immunology
    Human CXCR2 mRNA encodes the human C-X-C motif chemokine receptor 2 (CXCR2) protein, a member of the G-protein-coupled receptor family. CXCR2 is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system. This receptor also binds to chemokine (C-X-C motif) ligand 1 (CXCL1/MGSA), a protein with melanoma growth stimulating activity, and has been shown to be a major component required for serum-dependent melanoma cell growth.
    Human CXCR2 mRNA
  • HY-117403

    Cannabinoid Receptor Potassium Channel
    AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC50 values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms .
    AB-FUBICA
  • HY-P0049A

    Arg8-vasopressin diacetate; AVP diacetate; ADH

    Apoptosis Vasopressin Receptor Neurological Disease Cancer
    Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. Argipressin (diacetate) (AVP (diacetate)) can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). Argipressin (diacetate) (AVP (diacetate)) also have potentially important effects on centrally regulated metabolic processes .
    Argipressin diacetate

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