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G_i proteins

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36

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10

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112779
    Pertussis Toxin

    		Endogenous Metabolite Infection
    Pertussis Toxin is a protein-based AB5-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough. Pertussis Toxin inhibits G protein-coupled receptor (GPR) signaling through Gi proteins .
    Pertussis Toxin
  • HY-114364
    UDP-Galactose disodium
    4 Publications Verification

    		 Endogenous Metabolite P2Y Receptor Metabolic Disease
    UDP-Galactose disodium is a monosaccharide and a key glycosyl donor molecule in cells that participates in nucleotide sugar metabolism. UDP-Galactose disodium is the natural agonist of the P2Y14 receptor coupled to Gi proteins in the immune system (IC50 = 0.67 μM, hP2Y14). UDP-Galactose disodium can be used to study cell signal transduction and substance metabolism .
    UDP-Galactose disodium
  • HY-101213
    OSW-1
    5 Publications Verification

    		 Oxysterol-binding Protein-related Protein (ORP) Cancer
    OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of ooxysterol binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
    OSW-1
  • HY-P0172
    ATI-2341
    4 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
  • HY-W140439
    1-Oleoyl-sn-glycero-3-phosphocholine

    18:1 Lyso PC

    		 Endogenous Metabolite 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 .
    1-Oleoyl-sn-glycero-3-phosphocholine
  • HY-145404
    Mitragynine pseudoindoxyl
    1 Publications Verification

    		 Opioid Receptor Metabolic Disease
    Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .
    Mitragynine pseudoindoxyl
  • HY-137683A
    Guanosine 5'-O-2-thiodiphosphate trisodium

    GDPβS trisodium

    		 Adenylate Cyclase Cardiovascular Disease
    Guanosine 5'-O-(2-thiodiphosphate) trisodium (GDPβS trisodium) is a non-hydrolyzable derivative of GDP. Guanosine 5'-O-(2-thiodiphosphate) trisodium acts as an inhibitor of adenylyl cyclase (AC) with a Ki value of 600 nM. In the absence of glutamic-pyruvic transaminase (GPT) in cerebral cortex membranes of rodent models, Guanosine 5'-O-(2-thiodiphosphate) trisodium partially activates AC with an EC50 of 400 nM. Guanosine 5'-O-(2-thiodiphosphate) trisodium prevents norepinephrine-induced nitric oxide release in ventricular myocytes .
    Guanosine 5'-O-2-thiodiphosphate trisodium
  • HY-P0172A
    ATI-2341 TFA
    4 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-150524
    UDP-Galactose

    		Endogenous Metabolite P2Y Receptor Metabolic Disease
    UDP-Galactose is a monosaccharide and a key glycosyl donor molecule in cells that participates in nucleotide sugar metabolism. UDP-Galactose is the natural agonist of the P2Y14 receptor coupled to Gi proteins in the immune system (IC50 = 0.67 μM, hP2Y14). UDP-Galactose can be used to study cell signal transduction and substance metabolism .
    UDP-Galactose
  • 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-171978
    LM-189

    		Adrenergic Receptor Cardiovascular Disease
    LM-189 is a β2-adrenergic receptor (β2AR) ligand and G protein-biased modulator with a human β2AR Ki of 0.063 nM.LM-189 promotes β2AR coupling to Gαs and Gαi heterotrimers, stabilizes distinct β2AR conformations including a TM6 outward state, and increases β2AR ICL2 dynamics.LM-189 restricts β2AR ligand-binding pocket conformational heterogeneity, stabilizes polar ligand-receptor interaction networks, and exhibits bias toward Gαi signaling over Gαs signaling.LM-189 enabled cryo-EM structural characterization of the β2AR-Gi complex.LM-189 can be used for the research of congestive heart failure .
    LM-189
  • 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)
  • HY-P0142A
    DT-3 acetate

    		PKG Cardiovascular Disease
    DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
    DT-3 acetate
  • 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-170494
    AS-254s

    		Histone Methyltransferase Cancer
    AS-254s is the inhibitor for absent, small, or homeotic-like 1 protein (ASH1L) with an IC50 of 94 nM (FP assay). AS-254s exhibits antiproliferative activity against MLL1-rearranged leukemic cells with GI50 <1 μM. AS-254s induces the differentiation of MLL1-r leukemic cell .
    AS-254s
  • HY-N0927
    (-)-Isocorypalmine

    Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine

    		 Dopamine Receptor Others Neurological Disease
    (-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .
    (-)-Isocorypalmine
  • 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-P0142
    DT-3

    		PKG Cardiovascular Disease
    DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
    DT-3
  • HY-110202
    MRS5698

    		Adenosine Receptor Neurological Disease Inflammation/Immunology
    MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis .
    MRS5698
  • HY-114364S
    UDP-α-D-Galactose-13C disodium

    		Isotope-Labeled Compounds Others
    UDP-α-D-Galactose- 13C disodium is the 13C labeled UDP-α-D-Galactose disodium. UDP-Galactose disodium is a monosaccharide and a key glycosyl donor molecule in cells that participates in nucleotide sugar metabolism. UDP-Galactose disodium is the natural agonist of the P2Y14 receptor coupled to Gi proteins in the immune system (IC50 = 0.67 μM, hP2Y14). UDP-Galactose disodium can be used to study cell signal transduction and substance metabolism .
    UDP-α-D-Galactose-13C disodium
  • 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-174335
    UVI3502

    		Cannabinoid Receptor Neurological Disease
    UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases) .
    UVI3502
  • HY-173499
    HLDA-212

    		Aurora Kinase Apoptosis Cancer
    HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
    HLDA-212
  • HY-173003
    EP-3945

    		Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC50 for Gq being 211.6 nM .
    EP-3945
  • HY-W744699
    Larixol

    (+)-Larixol

    		 Src ERK Akt Inflammation/Immunology
    Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol 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. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
    Larixol
  • 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-151872
    HDAC-IN-48

    		HDAC Ferroptosis Cancer
    HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC-IN-48
  • HY-P1376A
    G-Protein antagonist peptide TFA
    1 Publications Verification

    		 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-163278
    Lck-IN-2

    		Src Apoptosis Cancer
    Lck-IN-2 (compound 12a) is an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck) with IC50 of 10.6 nM. Lck-IN-2 reveals efficacy in colon cancer cells with GI50s of 0.24-1.26 μM. Lck-IN-2 exhibits an apoptotic effect in Colo201 cells .
    Lck-IN-2
  • HY-W806047
    BRD4 Inhibitor-37

    		Epigenetic Reader Domain Cancer
    BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
    BRD4 Inhibitor-37
  • HY-170343
    PROTAC SMARCA2 degrader-32

    		PROTACs SWI/SNF Complex Cancer
    PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM . (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
    PROTAC SMARCA2 degrader-32
  • HY-145900
    S100A2-p53-IN-1

    		MDM-2/p53 Cancer
    S100A2-p53-IN-1 (compound 51) is a S100A2-p53 interactions inhibitor. S100A2 is a Ca 2+ binding protein with implications in cell signaling and is known to be upregulated in pancreatic cancer. S100A2-p53-IN-1 can inhibit the growth of the MiaPaCa-2 pancreatic cancer cell line (GI 50 of 1.2-3.4 μM) .
    S100A2-p53-IN-1
  • 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-182723
    PSB-16671

    		GPR84 Cancer
    PSB-16671 is an allosteric agonist of GPR84. PSB-16671 recruits β-arrestins and couples to Gi, enhances the Gi activation potency of orthosteric agonists, and exerts a synergistic effect with orthosteric agonists. PSB-16671 promotes G protein activation and partial chemotaxis independent of GPR84 in mouse neutrophils, maintains the phagocytic function of macrophages against cancer cells without inducing receptor desensitization. PSB-16671 can be used in cancer-related research .
    PSB-16671
  • HY-179633
    ZLMT-72

    		CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP Cancer
    ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC) .
    ZLMT-72
  • HY-181878
    Z8779877149

    Z7149

    		 Serotonin Transporter Adrenergic Receptor 5-HT Receptor Neurological Disease
    Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .
    Z8779877149

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