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product name CHIR-99021 (CT99021) HCl


Description: CHIR-99021 (also called CT99021) HCl is the hydrochloride salt of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM in cell-free assays; CHIR-99021 was proved to promote self-renewal and maintain pluripotency of both B6 and BALB/c ES cells via stabilizing the downstream effectors like c-Myc and β -catenin. In J1 mESC cells, CHIR-99021 played an important role in maintaining the colony morphology as well as the self-renewal when combined with leukemia inhibitory factor (LIF). CHIR-99021 has shown to regulate multiple signaling pathways which involve Wnt/β-catenin, TGF-β, Nodal and MAPK, and the expression of epigenetic regulatory genes like Dnmt3.

Reference: PLoS One. 2013;8(3):e58501.



Molecular Weight (MW)

501.8
Formula

C22H18Cl2N8.HCl
CAS No.

252917-06-9 (free base)
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 93 mg/mL (185.33 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL (slightly soluble or insoluble)
Solubility (In vivo)

15% Captisol: 30 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423710

General 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.
Animal model Female db/db mice or male ZDF rats with type 2 diabetes
Formulation Formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.
Dosages 48 mg/kg
Administration Oral gavage
Reference [1] Ring DB, et al. Diabetes, 2003, 52(3), 588-595.

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