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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
25 Results for "
GSIS
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "GSIS" in MCE Product Catalog:
169
169 Publications Verification
Synonyms: GSI-IX
Research Areas:
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment .
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L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers .
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Cardiovascular Disease Apocynaceae Alkaloids Plants Disease Research Fields Indole Alkaloids Catharanthus roseus (L.) G. Don
Target:
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Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively .
Cat. No.: HY-175701
CAS No.: 2810808-95-6
Synonyms: RO7795081; RG6652
Target:
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CT-996 is an orally active GLP-1RA agonist with an EC50 of 0.49 nM. CT-996 reduces the recruitment of β-arrestin and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity .
Cat. No.: HY-13027G
CAS No.: 208255-80-5
Synonyms: GSI-IX (GMP)
Synonyms: GSI-953
Target:
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Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease .
Cat. No.: HY-18614
CAS No.: 209984-68-9
Target:
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LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC50=0.005-20 nM). LY900009 can be used for advanced cancer research .
Cat. No.: HY-14363
CAS No.: 1082058-99-8
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TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-158583
CAS No.: 2126038-97-7
Cat. No.: HY-158584
CAS No.: 1997286-67-5
Synonyms: 9Z-Octadecenoic acid, 12-carboxy-1-pentyldodecyl ester
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13-OAHSA is one of fatty acid esters of hydroxy fatty acids (FAHFAs). 13-OAHSA increases glucose-stimulated insulin secretion (GSIS) at a high glucose concentration .
Cat. No.: HY-158650
CAS No.: 2005487-34-1
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10-OAHSA is one of fatty acid esters of hydroxy fatty acids (FAHFAs). 10-POHSA increases glucose-stimulated insulin secretion (GSIS) at a high glucose concentration. 10-OAHSA reduces LPS (HY-D1056)-induced Tnf-α secretion in bone marrow-derived dendritic cells (BMDCs) .
Cat. No.: HY-Q40876
CAS No.: 445000-45-3
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BBT is an enhancer of impaired glucose-stimulated insulin secretion (GSIS). BBT exhibits anti-hyperglycemia activity, and protects β-cells from cytokine- or streptozotocin (STZ (HY-13753))-induced cell death in type 2 diabetes models. BBT acts function via cAMP/PKA and long-lasting (L-type) voltage-dependent Ca2+ channel/CaMK2 pathway .
Cat. No.: HY-164451
CAS No.: 362653-62-1
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GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 inhibits the attachment-free growth of pancreatic cancer cells by inhibiting Notch signaling .
Cat. No.: HY-117236
CAS No.: 443989-01-3
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GSI-136 is an inhibitor of γ-secretase with an IC50 of 3 nM. GSI-136 can lead to a dose-dependent reduction of Aβ40 levels in diethylamine-extracted brain homogenates of C57BL/6 mice. GSI-136 can be studied in medicinal chemistry and Alzheimer's disease research .
Cat. No.: HY-115606
CAS No.: 1135304-61-8
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ML007 is a selective antagonist targeting the neuron-specific potassium-chloride co-transporter 2 (KCC2) with an IC50 for KCC2 is 537 nM, while its inhibitory activity on KCC1 is extremely weak (IC50 > 50 μM). ML077 inhibits the chloride ion excretion function of KCC2, increasing the intracellular chloride ion concentration, thereby enhancing the depolarization mediated by chloride ion channels. ML007 can promote glucose-stimulated insulin secretion (GSIS) without relying on KATP channels. ML007 can be used to study the functions related to pain, epilepsy, and insulin secretion .
Cat. No.: HY-178967
Research Areas:
DRAK1/2-IN-2 (Compound Y17) is a DRAK1/2 inhibitor with IC50 values for DRAK2 and DRAK1 of 353.2 nM and 507.4 nM respectively. DRAK1/2-IN-2 can enhance mitochondrial membrane potential and glucose-stimulated insulin secretion (GSIS). DRAK1/2-IN-2 resists lipotoxicity-induced cell apoptosis. DRAK1/2-IN-2 significantly inhibits the secretion of pro-inflammatory cytokine IL-1β, thereby exerting an anti-inflammatory effect. DRAK1/2-IN-2 can significantly lower the blood glucose levels of mice. DRAK1/2-IN-2 can be used in diabetes research.
Cat. No.: HY-145428
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BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression .
Cat. No.: HY-158639
CAS No.: 2042646-31-9
Target:
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12-POHSA is one of fatty acid esters of hydroxy fatty acids (FAHFAs). 12-POHSA increases glucose-stimulated insulin secretion (GSIS) at a high glucose concentration .
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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
