GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥98%
Moligand™, ≥98% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Product description: CHIR-98014 is an effective GSK-3Α and GSK-3Β inhibitor with IC50 values of 0.65 nM and 0.58 NM respectively. GSK-3(glycogen synthase Kinase 3) is a serine/threonine protein kinase that plays a key role in many intracellular signaling pathways, including Cell Proliferation, migration, inflammation and immune response, glucose regulation and apoptosis. GSK-3 is reported to be abnormally expressed in a variety of diseases, including type 2 diabetes, Alzheimer’s Disease, inflammation, cancer and bipolar disorder. CHIR-98014 is an effective inhibitor of GSK-3 Α and GSK-3 β. In CHO-IR cells or primary rat hepatocytes expressing INSR, CHIR-98014 stimulated GS activity in a dose-dependent manner, 2-3 times higher than baseline level. Similarly, CHIR-98014 activates GS more than [1] in type I skeletal muscles from insulin-sensitive Lean Zucker rats and insulin-resistant ZDF rats. In mouse ES-D3 cells, CHIR-98014 significantly activates Wnt/beta-catenin signaling pathway by inhibiting GSK-3 after 48 and 72 hours of treatment. CHIR-98014(30 mg/kg) significantly reduced fasting hyperglycemia within 4 hours after Oral Administration, and improved glucose treatment during oral or intravenous administration in a mouse model with marked diabetes and insulin resistance (DB/DB) .
Product Application:
CHIR 98014 has been used for the generation of small molecules neural progenitor cells and differentiation towards motor neurons. It has also been used as a Wnt/β-catenin pharmacological agonist in the cell-conditioned medium to perform chromatin immunoprecipitation (ChIP) studies in HT22 neurons.
Highly potent and selective GSK-3 inhibitor (IC50values are 0.58 and 0.65 nM for the β and α isoforms, respectively). Exhibits >500-fold selectivity for GSK-3β over a range of other kinases. Improves insulin sensitivity of muscle strips from diabetic rats
Condiciones de almacenamiento de almacenamiento
Store at -20°C
Enviado en
Ice chest + Ice pads
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta
This compound belongs to the class of organic compounds known as phenylpyrimidines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrimidine ring through a CC or CN bond. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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