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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
9 Results for "
Gαs protein
" in MedChemExpress (MCE) Product Catalog:
Products (9)
9 Results for "Gαs protein" in MCE Product Catalog:
7
7 Cited Publications
Target:
Research Areas:
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
Cat. No.: HY-171978
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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 .
Cat. No.: HY-162734
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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 .
Cat. No.: HY-112461
CAS No.: 389142-38-5
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NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 is a Gsα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
Cat. No.: HY-W041308
CAS No.: 64359-81-5
Synonyms: Kathon 930
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DCOIT (Kathon 930) is an isothiazolinone biocide and environmental pollutant that directly binds to G protein α subunits, with KD values of 0.92 mM and 0.4 mM for Gαs and Gαi, respectively. Binding of DCOIT to Gαi enhances the interaction between Gαi and mitochondrial calcium uniporter (MCU), alters the subcellular distribution of intracellular Ca 2+, and activates PKC/MEK/ERK signaling. DCOIT upregulates CYP19a transcription and aromatase activity, thereby disrupting steroid hormone homeostasis. DCOIT is used in studies of reproductive endocrine disruption and environmental toxicology .
Cat. No.: HY-162735
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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 .
Cat. No.: HY-W041308R
CAS No.: 64359-81-5
Synonyms: Kathon 930 (Standard)
Research Areas:
DCOIT (Standard) (Kathon 930 (Standard)) is the analytical standard of DCOIT (HY-W041308). This product is intended for research and analytical applications. DCOIT (Kathon 930) is an isothiazolinone biocide and environmental pollutant that directly binds to G protein α subunits, with KD values of 0.92 mM and 0.4 mM for Gαs and Gαi, respectively. Binding of DCOIT to Gαi enhances the interaction between Gαi and mitochondrial calcium uniporter (MCU), alters the subcellular distribution of intracellular Ca 2+, and activates PKC/MEK/ERK signaling. DCOIT upregulates CYP19a transcription and aromatase activity, thereby disrupting steroid hormone homeostasis. DCOIT is used in studies of reproductive endocrine disruption and environmental toxicology .
Cat. No.: HY-183400
CAS No.: 195450-11-4
Target:
Neurotensin Receptor MMP EGFR Toll-like Receptor (TLR) Wnt Caspase PARP MyD88 NF-κB TNF Receptor Apoptosis
Research Areas:
BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia .
Cat. No.: HY-182271
Research Areas:
GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia .
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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
