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CHIR-99021

Cat. No. M1692
CHIR-99021 Structure
Synonym:

CT99021; Laduviglusib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 50  USD50 In stock
5mg USD 75  USD75 In stock
10mg USD 100  USD100 In stock
50mg USD 260  USD260 In stock
100mg USD 520  USD520 In stock
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Quality Control & Documentation
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.

Product Citations
Customer Product Validations & Biological Datas
Source Sci Rep (2015). Figure 3. CHIR-99021
Method qPCR
Cell Lines J1 mESCs and F9 mEC cells
Concentrations 3 μM
Incubation Time 24 h
Results By contrast, all of the ESCC miRNAs were downregulated by CHIR (Fig. 3a–e). The miR-200b-429 and miR-183-182 clusters, which are highly expressed in pluripotent cells, were downregulated by both BIO and CHIR (Fig. 3f, 3g).
Source Sci Rep (2015). Figure 1. CHIR-99021
Method immunofluorescence staining
Cell Lines J1 mESCs and F9 mEC cells
Concentrations 3 μM
Incubation Time 24 h
Results The relativemRNA expression level of Nanog was determined in response to BIO or CHIR in J1mESCs and F9mEC cells by qPCR. As expected, transcription of Nanog in J1 mESCs and F9 mEC cells was upregulated by both BIO and CHIR
Protocol (for reference only)
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
Chemical Information
Molecular Weight 465.34
Formula C22H18Cl2N8
CAS Number 252917-06-9
Solubility (25°C) DMSO 16 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Ye, et al. PLoS One. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains.

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Keywords: CHIR-99021, CT99021; Laduviglusib supplier, GSK-3, inhibitors, activators


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