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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.
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Application | immunofluorescence staining |
| 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 |
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Application | qPCR |
| 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). |
| 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 |
| 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 |
| Best-selling GSK-3 Products |
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| CHIR-99021 HCl
CHIR-99021 HCl (Laduviglusib; CT99021) is a hydrochloride of CHIR-99021, with IC50 of 10 nM and 6.7 nM for GSK-3α and GSK-3β, respectively. |
| SB 216763
SB 216763 is a potent and selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM for GSK-3α. |
| TWS119
TWS119 is a GSK-3β inhibitor with IC50 of 30 nM. |
| CHIR 99021 trihydrochloride
Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. |
| BIO
BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific GSK-3 inhibitor, the IC50 acting on GSK-3α/β in cell-free assays is 5 nM, which is more than 16 times more selective than ACTing on CDK5. It is also a pan-JAK inhibitor with an IC50 value of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. |
| DIF-3
DIF-3 inhibits cell cycle by inducing G0/G1 arrest. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. |
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| AZD2858
AZD2858 is a potent, orally bioactive inhibitor of GSK-3 with an IC50 of 68 nM. |
| Indirubin
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of ~75 nM and 0.19 μM. |
| CHIR-98014
CHIR-98014 is a potent and selective GSK-3 inhibitor for GSK-3ɑ and GSK-3β with IC50 of 0.65 nM and 0.58 nM, respectively. |
| Tideglusib
Tideglusib (NP031112, NP-12) is a potent non ATP-competitive inhibitor of GSK3 with IC50 of 60 nM. |
| 1-Azakenpaullone
1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. |
| AR-A014418
AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM, without significant inhibition on 26 other kinases tested. |
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