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CHIR-99021

Cat. No. M1692
CHIR-99021 Structure
Synonym:

CT99021

Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 130 In stock
50mg USD 300 In stock
100mg USD 580 In stock
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Quality Control
Biological Activity

CHIR-99021 (CT99021) inhibits glycogen synthase kinase-3β (GSK3β, IC50 = 6.7 nm) and GSK3α (IC50 = 10 nm), inhibits preadipocyte differentiation (IC50 = 0.3 µM), possibly by blocking induction of C/EBPα and PPARγ, and mimics Wnt signaling in 3T3-L1 preadipocytes. CHIR99021 activates glycogen synthase in CHO-IR cells with EC50 of 763 nM. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) with 350-fold selectivity toward GSK-3β compared to CDKs.

Protocol
Cell Experiment
Cell lines J1 mESCs or F9 mEC cells
Preparation method Immunofluorescence staining The expression and subcellular localisation of β-catenin in J1 mESCs treated with 1 μM BIO or 3 μM CHIR for 24 h was detected by immunofluorescence staining. Nuclei were stained with DAPI. J1 mESCs or F9 mEC cells were fixed and permeabilized using immunostaining fixation buffer and then blocked in blocking buffer (Beyotime Institute of Biotechnology). Subsequently, cells were incubated with the indicated primary antibody overnight at 4°C, followed by three washes with washing buffer (Beyotime Institute of Biotechnology) for 5 min and then incubation with an Alexa Fluor 555-conjugated secondary antibody for 2 h at room temperature. Nuclei were stained with DAPI. Cells were photographed under an inverted fluorescence microscope (Nikon, Tokyo, Japan).
Concentrations 3µM
Incubation time 24h
Animal Experiment
Animal models Akita type 1 diabetic mice and wild-type mice
Formulation DMSO
Dosages 50 mg/kg, daily
Administration Intraperitoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 465.34
Formula C22H18Cl2N8
CAS Number 252917-06-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains.
Ye, et al. PLoS One. 2012;7(4):e35892. PMID: 22540008.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CHIR-99021, CT99021 supplier, GSK-3, inhibitors

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