Free shipping on all orders over $ 500


Cat. No. M1692
CHIR-99021 Structure


Size Price Availability Quantity
2mg USD 37.8  USD42 In stock
5mg USD 64.8  USD72 In stock
10mg USD 91.8  USD102 In stock
50mg USD 283.5  USD315 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

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
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 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.

Chemical Information
Molecular Weight 465.34
Formula C22H18Cl2N8
CAS Number 252917-06-9
Purity 99.66%
Solubility DMSO 16 mg/mL
Storage at -20°C

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.

Related GSK-3 Products

TSPC (HUN86320) is a Glycogen Synthase Kinase-​3β Inhibitor (GSK-3β Inhibitor).


BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively.


BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM.


Indirubin-3'-monoxime is a potent GSK-3β inhibitor with IC50 of 22 nM, and inhibits Cdk5/p35, Cdk1/cyclin-B and Cdk2/cyclin-E with IC50s of 100, 180, 250 nM.


Bikinin is a strong activator of brassinosteroid (BR) signaling.

Abmole Inhibitor Catalog 2017

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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.