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Pathways Recommended: GPCR/G Protein
Results for "

G protein inhibitor

" in MedChemExpress (MCE) Product Catalog:

428

Inhibitors & Agonists

5

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1

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5

Biochemical Assay Reagents

29

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1

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2

Inhibitory Antibodies

41

Natural
Products

5

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5

Isotope-Labeled Compounds

1

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4

Click Chemistry

3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-17561
    G-418 disulfate
    60+ Cited Publications

    Geneticin sulfate; Antibiotic G-418 sulfate

    		 Bacterial Antibiotic Infection
    G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells .
    G-418 disulfate
  • HY-130149
    Adagrasib
    55+ Cited Publications

    MRTX849

    		 Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
    Adagrasib
  • HY-12588
    Thiamet G
    45+ Cited Publications

    		 OGA Autophagy Cancer
    Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.
    Thiamet G
  • 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 .
    YM-254890
  • HY-N6791
    KT5823
    10+ Cited Publications

    		 PKA PKC Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation .
    KT5823
  • 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-17408
    Mevastatin
    5+ Cited Publications

    Compactin; ML236B

    		 HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic Infection Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment .
    Mevastatin
  • HY-158107
    BBO-8520
    1 Publications Verification

    		 Ras Cancer
    BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state. BBO-8520 can be used for the research of cancer .
    BBO-8520
  • HY-143589
    Glecirasib

    JAB-21822; KRAS G12C inhibitor 36

    		 Ras Cancer
    Glecirasib (Compound 1-2; JAB-21822) is an orally active and potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. Glecirasib has the potential for the research of KRAS G12C-mediated cancer .
    Glecirasib
  • HY-103450
    G36

    		Estrogen Receptor/ERR Endocrinology Cancer
    G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
    G36
  • HY-164607
    YL-5092

    		DNA/RNA Synthesis Apoptosis Cancer
    YL-5092 is a selective YT521-B homology (YTH) domain-containing protein 1 (YTHDC1) inhibitor with an IC50 of 7.4 nM and a KD of 29.6 nM. YL-5092 can suppress cancer cell proliferation and induce cell G0/G1 phase arrest and apoptosis. YL-5092 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
    YL-5092
  • HY-162289
    FAZ-3780
    2 Publications Verification

    		 DNA/RNA Synthesis Neurological Disease Cancer
    FAZ-3780 is an inhibitor that binds to the NTF2L domain of G3BP1/2. FAZ-3780 binds to the NTF2L nsP3 of G3BP1 with high affinity, with a Kd of 0.15 μM and a Pep-FRET IC50 of 0.7 μM. FAZ-3780 targets the protein-protein interaction domain of G3BP1/2, and specifically inhibits the co-condensation of G3BP1, caprin 1 and RNA in vitro. FAZ-3780 inhibits stress granule formation and disassembles pre-formed stress granules. FAZ-3780 can be used in studies related to cancer and neurodegenerative diseases .
    FAZ-3780
  • HY-15221
    Methylstat
    3 Publications Verification

    		 Apoptosis Histone Demethylase MDM-2/p53 Cardiovascular Disease Cancer
    Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
    Methylstat
  • HY-131649
    Compound C108
    1 Publications Verification

    		 DNA/RNA Synthesis Cancer
    Compound C108 is a G3BP2 inhibitor. Compound C108 also targeted stress granule-associated proteins and Gtpase-activating protein (SH3 domain) binding protein 2. Compound C108 potently inhibits esophageal squamous cell carcinoma (ESCC) cell metastasis .
    Compound C108
  • HY-137497
    KRAS inhibitor-9

    		Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
    KRAS inhibitor-9
  • HY-150147
    CAM833
    1 Publications Verification

    		 RAD51 Apoptosis Cancer
    CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a Kd of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .
    CAM833
  • HY-128522
    ARS-1323-alkyne

    		Ras Cancer
    ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
    ARS-1323-alkyne
  • HY-17561R
    G-418 disulfate (Standard)

    Geneticin sulfate (Standard); Antibiotic G-418 sulfate (Standard)

    		 Reference Standards Bacterial Antibiotic Infection
    G-418 (disulfate) (Standard) is the analytical standard of G-418 (disulfate). This product is intended for research and analytical applications. G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells[1].
    G-418 disulfate (Standard)
  • HY-14987
    AX20017
    2 Publications Verification

    		 Bacterial Infection
    AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.
    AX20017
  • HY-18707
    K-Ras(G12C) inhibitor 12

    		Ras Apoptosis Cancer
    K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
    K-Ras(G12C) inhibitor 12
  • HY-10499
    PH-064
    2 Publications Verification

    BIM-46187

    		 Serotonin Transporter Akt Neurological Disease Inflammation/Immunology Cancer
    PH-064 (BIM-46187) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 has potent anti-hyperalgesia activity. PH-064 inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury .
    PH-064
  • HY-16642A
    LY2828360
    1 Publications Verification

    		 Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
    LY2828360
  • HY-U00431
    CCG 203769

    		RGS Protein Neurological Disease
    CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
    CCG 203769
  • HY-144661
    KRAS G12D inhibitor 14

    		Ras Apoptosis Cancer
    KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D .
    KRAS G12D inhibitor 14
  • HY-153821
    PROTAC KRAS G12C degrader-2

    		Ras PROTACs Cancer
    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
    PROTAC KRAS G12C degrader-2
  • HY-115449
    Chromeceptin
    2 Publications Verification

    94G6

    		 IGF-1R Akt mTOR Cancer
    Chromeceptin (94G6) is an IGF signaling pathway inhibitor. Chromeceptin suppresses IGF2 expression at mRNA and protein levels in hepatocyte and HCC cells. Chromeceptin inhibits the phosphorylation levels of AKT and mTOR .
    Chromeceptin
  • HY-171656
    G721-0282

    		Glycosidase NF-κB COX STAT ERK p38 MAPK Apoptosis CDK Survivin Bcl-2 Family Neurological Disease Inflammation/Immunology Cancer
    G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer .
    G721-0282
  • HY-W100287
    Murrayafoline A

    		NF-κB p38 MAPK Interleukin Related IKK JNK β-catenin Wnt Neurological Disease Inflammation/Immunology Cancer
    Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer .
    Murrayafoline A
  • HY-112591
    NSC260594

    XMH95

    		 Apoptosis HIV Wnt Bcl-2 Family Cancer
    NSC260594 induces Apoptosis. NSC260594 binds the shallow groove of the Mcl-1 protein, and inhibits Mcl-1 expression through down-regulation of Wnt signaling proteins. NSC260594 can also recognize G9-G10-A11-G12 RNA tetraloop of HIV and prevent the binding of the Gag protein within the 5’-UTR. NSC260594 inhibits tumor growth, and can be used for research of Triple-negative breast cancers (TNBCs) .
    NSC260594
  • HY-12372
    Sanggenon G

    		IAP Caspase Cancer
    Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation .
    Sanggenon G
  • HY-44062
    G9a-IN-1

    		Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
    G9a-IN-1
  • HY-146887
    USP7-IN-9

    		Deubiquitinase Apoptosis Cancer
    USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21 .
    USP7-IN-9
  • HY-163707
    UR778Br

    		Apoptosis Cancer
    UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .
    UR778Br
  • HY-149891
    HSP90-IN-23

    		HSP Cancer
    HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
    HSP90-IN-23
  • HY-120444
    MS0124

    		Histone Methyltransferase Cancer
    MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM for GLP and G9a,respectively .
    MS0124
  • HY-W747572
    (+)-Perillyl alcohol

    (R)-(+)-Perillyl alcohol

    		 Ras Cancer
    (+)-Perillyl alcohol is the enantiomer of S-(-)-Perillyl alcohol (HY-116514). (+)-Perillyl alcohol can inhibit the growth of polypeptides and block the cell cycle in the G0/G1 phase. (+)-Perillyl alcohol induces cell signaling that is associated with changes in cytoskeletal actin organization and reduced protein expression of growth regulatory proteins such as Ras and CDC2 kinase .
    (+)-Perillyl alcohol
  • HY-123520
    GSK299115A

    		G Protein-coupled Receptor Kinase (GRK) PKA Cancer
    GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor .
    GSK299115A
  • HY-W036034A
    GRK-IN-1

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
    GRK-IN-1
  • HY-146302
    14-3-3η Protein inhibitor 1
    2 Publications Verification

    		 Apoptosis Cancer
    14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
    14-3-3η Protein inhibitor 1
  • HY-143603
    KRAS G12D inhibitor 10

    		Ras Cancer
    KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34) .
    KRAS G12D inhibitor 10
  • HY-143607
    KRAS G12D inhibitor 13

    		Ras Cancer
    KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142) .
    KRAS G12D inhibitor 13
  • HY-153413
    Kras4B G12D-IN-1

    		Ras Cancer
    Kras4B G12D-IN-1 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566) .
    Kras4B G12D-IN-1
  • HY-176279
    Hsp90-IN-42

    		HSP Cancer
    Hsp90-IN-42 (Compound 13l) is a potent heat shock protein 90 (Hsp90) inhibitor (IC50=15.65 nM). Hsp90-IN-42 reduces the stability of the epidermal growth factor receptor (EGFR), suppressing the activation of the EGFR-Akt signaling pathway, inducing G0/G1 phase arrest in colorectal cancer cells (such as HT-29 cells), and slightly triggering apoptosis. Hsp90-IN-42 also inhibits cell proliferation and migration by down-regulating the expression of CDK12, CDK13, and Bcl-2 proteins, and up-regulating the expression of Bax protein. Hsp90-IN-42 is promising for research of colorectal cancer .
    Hsp90-IN-42
  • HY-149720
    GRL018-21

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 value of 10 nM .
    GRL018-21
  • HY-17660
    G923-0271

    		DNA/RNA Synthesis Neurological Disease
    G923-0271 is a TDP-43 protein inhibitor. G923-0271 can be used for the research of neurological disease, such as Alzheimer's Disease .
    G923-0271
  • HY-P3786
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH

    		PKA PKC Cancer
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor .
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH
  • HY-143606
    KRAS G12D inhibitor 12

    		Ras Cancer
    KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134) .
    KRAS G12D inhibitor 12
  • HY-143604
    KRAS G12D inhibitor 11

    		Ras Cancer
    KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 11 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 52) .
    KRAS G12D inhibitor 11
  • HY-143599
    KRAS G12D inhibitor 8

    		Ras Cancer
    KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2) .
    KRAS G12D inhibitor 8
  • HY-171047
    Autophagy inducer 7

    		Apoptosis Autophagy DNA/RNA Synthesis Akt mTOR Cancer
    Autophagy inducer 7 (Compound SSA) is an Autophagy and Apoptosis inducer. Autophagy inducer 7 activates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Autophagy inducer 7 suppresses DNA synthesis and causes a G0-G1 cell-cycle arrest. Autophagy inducer 7 inhibits tumor cell growth .
    Autophagy inducer 7

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