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Pathways Recommended: GPCR/G Protein MAPK/ERK Pathway Neuronal Signaling JAK/STAT Signaling
Results for "

G protein signaling pathway

" in MedChemExpress (MCE) Product Catalog:

79

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1

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1

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7

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1

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12

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4

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111557
    YM-254890
    Maximum Cited Publications
    17 Publications Verification

    		 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-B1142
    Lipoamide
    5+ Cited Publications

    (±)-α-Lipoamide; DL-Lipoamide; DL-6,8-Thioctamide

    		 NO Synthase Others
    Lipoamide ((±)-α-Lipoamide) is a monocarboxylic acid derivative of a neutral amide, formed by the condensation of the carboxyl group of lipoic acid and ammonia. Lipoamide protects against oxidative stress-mediated neuronal cell damage and also acts as a coenzyme to transfer acetyl groups and hydrogen during pyruvate deacylation. Lipoamide also stimulates mitochondrial biogenesis in adipocytes through the endothelial NO synthase-cGMP-protein kinase G signaling pathway .
    Lipoamide
  • HY-100355
    C18-Ceramide (d18:1/18:0)

    C18-Ceramide

    		 Endogenous Metabolite Neurological Disease Cancer
    C18-Ceramide (d18:1/18:0) is a bioactive molecule with multiple functions in cells, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology .
    C18-Ceramide (d18:1/18:0)
  • HY-139214
    IXA4
    5+ Cited Publications

    		 IRE1 Neurological Disease
    IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation .
    IXA4
  • HY-147245
    Basroparib

    STP1002

    		 PARP Cancer
    Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors .
    Basroparib
  • HY-W013706
    Inosine-5'-triphosphate trisodium salt

    ITP trisodium salt; Inosine triphosphate trisodium salt

    		 Endogenous Metabolite Metabolic Disease
    Inosine-5'-triphosphate trisodium salt is a nucleotide analogue that acts on multiple G proteins and is widely used in G protein-related research. It can bind to the α -subunit of G proteins and participate in G protein-mediated signal transduction as a substitute for GTP. Its mechanism of action is to interact with the nucleotide-binding site of the G protein α -subunit, affecting the activity and function of G proteins. In the research field, it is mainly used to explore the role of the G protein signaling pathway in cellular physiological and pathological processes. For example, in HL-60 leukemia cells, its impact on G protein-mediated signal transduction can be studied .
    Inosine-5'-triphosphate trisodium salt
  • HY-N0837
    Veratramine
    1 Publications Verification

    NSC17821; NSC23880

    		 PI3K Akt mTOR Autophagy Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
    Veratramine
  • HY-159788
    PROTAC K-Ras Degrader-4

    		PROTACs Ras Cancer
    PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for KRAS that degrades KRAS G12D in GP5d and degrades KRAS G12V in cell SW620 with DC50s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway . (Pink: ligand for target protein pan-KRAS degrader 1 (HY-162960); Black: linker (HY-159790); Blue: ligand for E3 ligase VHL (HY-W998248))
    PROTAC K-Ras Degrader-4
  • HY-N6588
    3,4,5-Tricaffeoylquinic acid

    3,4,5-triCQA

    		 Akt NF-κB Inflammation/Immunology Cancer
    3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .
    3,4,5-Tricaffeoylquinic acid
  • HY-W355700
    1-Oleoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine

    		Drug Metabolite Infection
    1-oleoyl-sn-glycero-3-phosphoethanolamine (LysoPE 18:1) is a lysophosphatidylethanolamine molecule involved in phospholipid metabolism, targeting cell membrane receptors (such as G protein-coupled receptors) to regulate cell signaling pathways. 1-oleoyl-sn-glycero-3-phosphoethanolamine may activate mitogen-activated protein kinase (MAPK) signaling, promote cell migration, regulate inflammatory responses and lipid metabolism, and has both pro-inflammatory and anti-inflammatory activities. 1-oleoyl-sn-glycero-3-phosphoethanolamine is mainly used in the screening of biomarkers for metabolic diseases (such as non-alcoholic fatty liver disease and obesity), as well as the study of the mechanism of lysophospholipids in cell membrane homeostasis and signal transduction .
    1-Oleoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine
  • 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-N3097
    Pellitorine

    		TRP Channel Amyloid-β Toll-like Receptor (TLR) Keap1-Nrf2 Heme Oxygenase (HO) Dihydroorotate Dehydrogenase Ferroptosis PAI-1 NF-κB ERK Proton Pump Glutathione Peroxidase Thrombin Insecticide Bacterial Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria .
    Pellitorine
  • HY-165428
    SCH-900875

    		CXCR Arrestin Inflammation/Immunology
    SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease) .
    SCH-900875
  • HY-136832
    Noribogaine hydrochloride

    		Serotonin Transporter Potassium Channel Arrestin Opioid Receptor Cardiovascular Disease Neurological Disease
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .
    Noribogaine hydrochloride
  • HY-107580
    GPR109 receptor agonist-1

    		GPR109A Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    GPR109 receptor agonist-1 is a highly selective agonist of the human orphan G protein-coupled receptor GPR109b, and does not activate the mouse homologous receptor PUMA-G. GPR109 receptor agonist-1 functionally modulates the human GPR109b receptor via the cAMP signaling pathway, with an EC50 of 400 nM. GPR109 receptor agonist-1 inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors. GPR109 receptor agonist-1 can be used in studies related to dyslipidemia and atherosclerosis .
    GPR109 receptor agonist-1
  • HY-122620
    Rafutrombopag (tautomerism)

    Hetrombopag (tautomerism); SHR-8735 (tautomerism)

    		 Thrombopoietin Receptor STAT PI3K ERK Apoptosis CDK Cardiovascular Disease Inflammation/Immunology
    Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
    Rafutrombopag (tautomerism)
  • HY-14604
    Xaliproden hydrochloride
    1 Publications Verification

    SR57746A; SR57746 hydrochloride

    		 5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK Neurological Disease Metabolic Disease
    Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
    Xaliproden hydrochloride
  • HY-167856
    RTI-122

    		GPR88 Neurological Disease
    RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
    RTI-122
  • 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-120967
    (2S)-OMPT triethylamine, in ethanol:chloroform (1:1), 98%

    		p38 MAPK Akt Interleukin Related Cancer
    (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98%, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% can be used for the research of ovarian cancer .
    (2S)-OMPT triethylamine, in ethanol:chloroform (1:1), 98%
  • HY-162734
    BRD5075

    		GPR65 Inflammation/Immunology
    BRD5075 is a selective GPR65 activator. BRD5075 enhances GPR65 activity under acidic conditions, promotes Gαs-dependent signaling pathways, including cAMP production and G protein recruitment. BRD5075 regulates the cytokine and chemokine expression network in dendritic cells, and inhibits the expression of pro-inflammatory cytokines and chemokines in a GPR65-dependent manner. BRD5075 is applicable to research related to inflammatory bowel disease .
    BRD5075
  • HY-150795
    SY-LB-35

    		TGF-beta/Smad PI3K Akt ERK JNK Others
    SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways .
    SY-LB-35
  • 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-120967A
    (2S)-OMPT

    		p38 MAPK Akt Interleukin Related Cancer
    (2S)-OMPT, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT can be used for the research of ovarian cancer .
    (2S)-OMPT
  • HY-U00416
    ARS-1323

    		Ras Cancer
    ARS-1323 is a KRAS G12C inhibitor. ARS-1323 specifically binds to the cysteine residue on the mutant K-Ras protein, locks it in the GDP-bound conformation, thereby blocking K-Ras activation and downstream signaling pathways. ARS-1323 can be used to investigate the signal transduction mechanisms and growth characteristics of tumor cells driven by K-Ras G12C .
    ARS-1323
  • 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-P3136
    TRV055

    TRV120055

    		 Angiotensin Receptor ERK Cardiovascular Disease
    TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses [1]
    TRV055
  • HY-173178
    LNS8801

    		Estrogen Receptor/ERR Cancer
    LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes .
    LNS8801
  • HY-P10489
    Kisspeptin-14 human

    		Kisspeptin Receptor Cancer
    Kisspeptin-14 human is a peptide hormone encoded by the KiSS-1 gene. Kisspeptin-14 human, along with several other similar peptide hormones, is produced from a common precursor protein by cleavage by different proteases. Kisspeptin-14 human is an endogenous ligand of KISS1R. Kisspeptin-14 human has the same receptor binding efficiency and potency as full-length kisspeptin. Kisspeptin-14 human binds to its receptor GPR54 and is able to activate this G protein-coupled receptor and activate multiple intracellular signaling pathways. Kisspeptin-14 human can be used to study reproductive development and tumor metastasis .
    Kisspeptin-14 human
  • HY-120006A
    (rel)-AR234960
    1 Publications Verification

    		 ERK Cardiovascular Disease
    (rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS. (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor (CTGF) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor. (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure .
    (rel)-AR234960
  • HY-145589
    Rafutrombopag

    Hetrombopag; SHR-8735

    		 Thrombopoietin Receptor STAT PI3K ERK Apoptosis CDK Cardiovascular Disease Inflammation/Immunology Cancer
    Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
    Rafutrombopag
  • HY-163671
    PW0729

    		GPR52 Arrestin Neurological Disease
    PW0729 is a selective GPR52 agonist. PW0729 activates G protein/cAMP signaling pathway, with bias toward this pathway over β-arrestin recruitment, and induces GPR52 desensitization. PW0729 can be used for the research of neuropsychiatric and neurological diseases .
    PW0729
  • HY-P3136A
    TRV055 hydrochloride

    TRV120055 hydrochloride

    		 Angiotensin Receptor Cardiovascular Disease
    TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses [1]
    TRV055 hydrochloride
  • HY-162735
    BRD5080

    		GPR65 Inflammation/Immunology
    BRD5080 is a GPR65 agonist. BRD5080 activates GPR65 to enhance the cAMP signaling pathway, reduce the expression of inflammatory cytokines and chemokines in dendritic cells, enhance the activity of human wild-type, mouse wild-type, and human GPR65 I231L variant receptors in a pH-dependent manner, and mediate the recruitment of Gαs protein. BRD5080 can be used in the research of inflammatory bowel disease .
    BRD5080
  • HY-135564A
    RK-682

    		Phosphatase Phospholipase HIV Protease ERK Autophagy Infection Cancer
    RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 .
    RK-682
  • HY-110302
    6'-GNTI dihydrochloride

    		Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
    6'-GNTI dihydrochloride
  • 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-N0837R
    Veratramine (Standard)

    NSC17821 (Standard); NSC23880 (Standard)

    		 Reference Standards PI3K Akt mTOR Autophagy Apoptosis Neurological Disease Metabolic Disease Cancer
    Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
    Veratramine (Standard)
  • HY-179520
    XSJ151

    		Topoisomerase DNA/RNA Synthesis MDM-2/p53 Bcl-2 Family Cancer
    XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer .
    XSJ151
  • HY-E70678
    CDK3/CycE1 Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycE1 Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycE1 Recombinant Human Active Protein Kinase
  • HY-171788
    NMT-IN-8

    		N-myristoyltransferase Cancer
    NMT-IN-8 (Compound Ex.129) is an orally active and highly selective inhibitor of N-myristoyl transferase (NMT) with an IC50 value of ＜10 nM. NMT-IN-8 binds to the peptide binding pocket of NMT, blocking its catalyzed protein N-myristoylation to interfere with key pathways such as protein trafficking, signal transduction, and viral replication. NMT-IN-8 is promising for research of oncology (e.g., MYC-addicted cancers, B-cell lymphoma) and infectious diseases (e.g., malaria, HIV, rhinovirus infection) .
    NMT-IN-8
  • HY-176288
    eIF4E/eIF4G PPI-IN-1

    		Eukaryotic Initiation Factor (eIF) Bcl-2 Family Apoptosis Ras PERK Cancer
    eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice .
    eIF4E/eIF4G PPI-IN-1
  • HY-113225B
    Guanosine triphosphate tritris

    GTP tritris

    		 Endogenous Metabolite Exosomes Cancer
    Guanosine triphosphate tritris (GTP tritris) serves as a vital enhancer of myogenic cell differentiation and plays a critical role in modulating miRNA-myogenic regulator factors. It also facilitates the release of exosomes enriched with guanosine and guanosine-derived molecules, and is regarded as an activated precursor for RNA synthesis. In mitochondrial function, GTP participates in the import of proteins into the matrix, which is essential for various regulated pathways, and is involved in initiating peptide synthesis through the binding of formylmethionyl-tRNA to the ribosome, as well as polypeptide chain elongation. Additionally, GTP acts as a phosphate and pyrophosphate carrier that channels chemical energy into specific biosynthetic pathways. It activates signal transducing G proteins that regulate cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases, including Ras and Rho, is integral to both proliferation and apoptosis. Furthermore, the small GTPase Rab is instrumental in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is an energy-rich precursor in the enzymatic biosynthesis of DNA and RNA.
    Guanosine triphosphate tritris
  • HY-168012
    Pan-RAS-IN-6

    		Ras Phosphatase Cancer
    Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
    Pan-RAS-IN-6
  • HY-168971
    Paeoniflorin-6′-O-benzene sulfonate

    CP-25

    		 IFNAR STAT TNF Receptor Interleukin Related CXCR JAK G Protein-coupled Receptor Kinase (GRK) Inflammation/Immunology
    Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model .
    Paeoniflorin-6′-O-benzene sulfonate
  • HY-E70677
    CDK3/CycC Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycC Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycC Recombinant Human Active Protein Kinase
  • HY-E70680
    CDK3/CycO Recombinant Human Active Protein Kinase

    		CDK Cancer
    CDK3 is a major player driving retinoblastoma (Rb) phosphorylation during the G0/G1 transition and in the early G1 phase of the cell cycle. CDK3 interacts with various transcription factors involved in cell proliferation, differentiation, and transformation driven by the EGFR/Ras signaling pathway. CDK3/CycO Recombinant Human Active Protein Kinase is an ortholog of CDK3 .
    CDK3/CycO Recombinant Human Active Protein Kinase
  • HY-107216A
    (3aS,4R,9bR)-G-1

    		Adhesion G Protein-coupled Receptors (AGPCRs) PI3K Neurological Disease Cancer
    (3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression .
    (3aS,4R,9bR)-G-1
  • HY-P11140
    KSL-W

    		Bacterial Reactive Oxygen Species (ROS) Infection Inflammation/Immunology
    KSL-W is a multifunctional antibacterial peptide with immune regulatory function. KSL-W has a chemotactic effect on neutrophils. KSL-W can induce neutrophil F-actin polymerization dependent on the Gαi protein signaling pathway. KSL-W can inhibit the production of reactive oxygen species (ROS) in neutrophils. KSL-W can be used for research on infection control and inflammation regulation .
    KSL-W
  • HY-106964A
    (Rac)-S 16924

    		5-HT Receptor Neurological Disease
    (Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia .
    (Rac)-S 16924

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