CHIR-99021 (CT99021) - Moligand™, 10mM in DMSO , Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1, CAS No.252917-06-9, Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1
CHIR-99021 (CT99021) - Moligand™, 10mM in DMSO , Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1, CAS No.252917-06-9, Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1
GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs 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 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
In vitro
CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM.
In vivo
Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge. Cell Data
cell lines：
Concentrations：0.01-10 μM
Incubation Time：30 min
Powder Purity:≥97%
Specifications
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR990
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of cyclin dependent kinase 1;Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of mitogen-activated protein kinase 1
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