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 |
| 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.
| Related GSK-3 Products |
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Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases. |
| FRATtide
FRATtide is a peptide derived from the GSK-3 binding protein that inhibits the phosphorylation of Axin and β-catenin. |
| ZDWX-25
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. |
| TC-G 24
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| SAR502250
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. |
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