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CHIR-98014 is a potent and selective human GSK-3 inhibitor for human GSK-3ɑ and human GSK-3β with IC50 of 0.65 and 0.58 nM, respectively. CHIR-98014 inhibits human GSK-3β with Ki values of 0.87 nM. Although CHIR-98014 serves as a simple competitive inhibitor of ATP binding, CHIR-98014 exhibits from 500-fold to <1000-fold selectivity for GSK-3 versus 20 other protein kinases including CDC2, erk2, tie2, KDR et al. CHIR-98014 prevents CDC2 with an IC50 of 3.7 μM.
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Source | Stem Cell Reports (2014). Figure 5. CHIR-98014 |
| Method | confocal microscopy | |
| Cell Lines | Cortical and hippocampal primary neuronal cells | |
| Concentrations | 10 μM | |
| Incubation Time | 12 h | |
| Results | Using confocal microscopy, we demonstrated that treatment of the cortical aswell as hippocampal neuronswith 10 μMCHIR98014 prevents loss of neurites caused by 20 μMPrP1–30 |
| Molecular Weight | 486.31 |
| Formula | C20H17Cl2N9O2 |
| CAS Number | 252935-94-7 |
| Solubility (25°C) | DMSO 4 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GSK-3 Products |
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| CHIR-99021
CHIR-99021 (CT99021) is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively. |
| 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. |
| 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. |
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