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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
166 Results for "
Transmembrane domain
" in MedChemExpress (MCE) Product Catalog:
Products (166)
166 Results for "Transmembrane domain" in MCE Product Catalog:
5
Category:
Natural Products Other disease Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields
Target:
3
3 Cited Publications
NBI-27914 is a highly selective, high-affinity non-peptide competitive antagonist of human corticotropin-releasing factor receptor 1 (CRFR1). NBI-27914 primarily binds to the His199 and Met276 sites in the transmembrane domain of the receptor .
2
2 Cited Publications
Cat. No.: HY-135416
CAS No.: 98072-47-0
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2
Taladegib is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC50 of 7.6 nM in CGNP cell proliferation assays. Taladegib binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib can be used in studies of Hedgehog pathway-related cancers .
2
2 Cited Publications
F7H is a Frizzled receptor FZD7 antagonist (IC50: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) .
2
2 Cited Publications
Cat. No.: HY-P1925A
CAS No.: 1222186-26-6
Research Areas:
1
1 Cited Publications
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NVS-STG2 is a molecular glue that targets STINGtransmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
1
1 Cited Publications
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AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
1
1 Cited Publications
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1
1 Cited Publications
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AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
Cat. No.: HY-P1985
CAS No.: 2408730-51-6
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GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) .
Cat. No.: HY-P2508
CAS No.: 149205-73-2
NSC49652 is a reversible, orally active p75 neurotrophin receptor (p75 NTR, also known as NGFR, TNFRSF16, and CD271) agonist. NSC49652 targets the transmembrane domain of p75 NTR. NSC49652 induces apoptosis and affects the viability of melanoma cells .
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TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
Cat. No.: HY-P10495A
Cat. No.: HY-119229
CAS No.: 815592-21-3
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VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and P-gp. VRT-325 promotes maturation of CFTR and P-gp processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis [1] [3].
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GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
Cat. No.: HY-178234
CAS No.: 1892576-07-6
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LY237 is a potent GPR84 full agonist, with EC50 values of 0.189 nM and 0.07 nM in cAMP inhibition assay and calcium flux assay, respectively. LY237 binds to the amphipathic orthosteric pocket of GPR84, stabilizes the active conformation of the receptor, and promotes its coupling with Gαi protein. LY237 can be used in research related to ulcerative colitis, fibrotic diseases, non-alcoholic steatohepatitis, and acute respiratory distress syndrome .
Cat. No.: HY-P10716
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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
