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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
89 Results for "
G protein signaling pathway
" in MedChemExpress (MCE) Product Catalog:
Products (89)
89 Results for "G protein signaling pathway" in MCE Product Catalog:
19
19 Publications Verification
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12
12 Cited Publications
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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 .
10
10 Cited Publications
Synonyms: (±)-α-Lipoamide; DL-Lipoamide; DL-6,8-Thioctamide
Category:
Human Gut Microbiota Metabolites Natural Products Other Diseases Endogenous metabolite Disease Research Fields
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2
2 Cited Publications
FzM1.8 is a Wnt/β-catenin signaling pathway agonist and an allosteric agonist of Frizzled 4 (FZD4), with a pEC50 of 6.4 for FZD4 . FzM1.8 stabilizes a conformation with increased affinity for heterotrimeric G proteins, promoting Gβγ release and subsequent PI3K activation. FzM1.8 activates the AKT pathway downstream of FZD4. FzM1.8 does not affect FZD4 maturation or plasma membrane localization and does not induce FZD4 endocytosis. FzM1.8 upregulates the WNT-responsive genes C-myc and Cyclin D1, while leaving lgr5 expression unchanged. FzM1.8 can be used for colon cancer research .
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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 .
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1
1 Cited Publications
Synonyms: SR57746A; SR57746 hydrochloride
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5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK
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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 .
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1 Cited Publications
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(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 .
1
1 Cited Publications
Cat. No.: HY-N0620
CAS No.: 102841-43-0
Category:
Alkaloids Neurological Disease Other Alkaloids Endogenous metabolite Disease Research Fields Cancer
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Synonyms: STP1002
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 .
Cat. No.: HY-W013706
CAS No.: 35908-31-7
Synonyms: ITP trisodium salt; Inosine triphosphate trisodium salt
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Cat. No.: HY-N6588
CAS No.: 86632-03-3
Synonyms: 3,4,5-triCQA
Cat. No.: HY-W355700
CAS No.: 89576-29-4
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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 .
Cat. No.: HY-N3097
CAS No.: 18836-52-7
Cat. No.: HY-165428
CAS No.: 907206-98-8
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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) .
Cat. No.: HY-136832
CAS No.: 110514-35-7
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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 .
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Research Areas:
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 .
Synonyms: Hetrombopag (tautomerism); SHR-8735 (tautomerism)
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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 .
Cat. No.: HY-167856
CAS No.: 3034664-39-3
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
