CHIR-99021 (CT99021) - 10mM in DMSO, high purity , CAS No.252917-06-9(DMSO)

Item Number
C408766
Grouped product items
SKUSizeAvailabilityPrice Qty
C408766-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$333.90

Basic Description

Specifications & Purity10mM in DMSO
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

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%

Associated Targets(Human)

CDK1 Tchem Cyclin-dependent kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GSK3B Tclin Glycogen synthase kinase-3 beta (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GSK3A Tclin Glycogen synthase kinase-3 alpha (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAPK1 Tchem Mitogen-activated protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES CC1=C[NH]C(=N1)C2=CN=C(NCCNC3=CC=C(C=N3)C#N)N=C2C4=CC=C(Cl)C=C4Cl
Molecular Weight 465.34

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 45 mg/mL (196.44 mM); Ethanol: 45 mg/mL (196.44 mM); Water: Insoluble;

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