G721-0377
G721-0377 is a CHI3L1 modulator with a human Kd value of 45 μM. G721-0377 binds to CHI3L1 and modulates downstream signaling pathways. G721-0377 suppresses CHI3L1-induced NF-κB activation, decreases secretion of CHI3L1 and IL-6. G721-0377 can be used for the research of Alzheimer's disease.
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- CAS. Nr.: 946336-44-3
- Formel: C22H25N5O4S
- Molecular Weight:455.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
NF-κB |
IL-6 |
In Vitro
G721−0377 binds to purified human CHI3L1 protein with a Kd of 45 μM[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h incubation) dose-dependently restores pHrodo-Aβ1-42 uptake in CHI3L1-treated human iPSC-derived astrocytes[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h cincubation) dose-dependently restores lysosomal proteolytic function (DQ-BSA degradation) in CHI3L1-treated human iPSC-derived astrocytes[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h incubation) dose-dependently restores lysosomal acidification in CHI3L1-treated human iPSC-derived astrocytes, with significant recovery observed at 25 and 50 μM[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h cincubation) dose-dependently suppresses CHI3L1 secretion in CHI3L1-treated human iPSC-derived astrocytes[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h cincubation) dose-dependently suppresses IL-6 secretion in CHI3L1-treated human iPSC-derived astrocytes[1].
G721−0377 (10-50 μM; 30 min pre-incubation; followed by 24 h cincubation) dose-dependently suppresses CHI3L1-induced NF-κB activation in human iPSC-derived astrocyte[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:human iPSC-derived astrocytes treated with recombinant CHI3L1
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Concentration:10 μM; 25 μM; 50 μM
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Incubation Time:30 min pre-incubation; followed by 24 h incubation
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Result:Robustly suppressed CHI3L1-induced CHI3L1 and IL-6 secretion in a dose-dependent manner, achieving statistically significant reduction at 10 μM and near-baseline levels at 50 μM, relative to CHI3L1-treated controls.
Chemical Information
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CAS. Nr. 946336-44-3
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Molecular Weight 455.53
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Formel C22H25N5O4S
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SMILES
CC(C)CC1=C(SCC(NC2=CC=C(C(N)=O)C=C2)=O)C3=C(N=C1)N(C)C(N(C)C3=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)