IM-12 is a potent and selective GSK-3β inhibitor with IC50 of 53 nM, which also enhances canonical Wnt signalling. IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and subsequently increases β-catenin concentration significantly in hNPCs. IM-12 significantly increased β-catenin levels. When used to treat human neural progenitor cells, IM-12 promoted neuronal differentiation resulting in an increase of neuronal cells. IM-12 has an IC50 of 53 nM in an in vitro binding assay, compared with 92 nM for SB-216763 in the same assay condition.
| Cell Experiment | |
|---|---|
| Cell lines | ReNcell VM cells |
| Preparation method | To measure viable cells, using CASY technology with the appropriate program to analyze 50-100 μL of cell suspension .Adding ReNcell VM cells are at a defined cell number and proliferated for 24 h. Then changing the medium to proliferation medium with added substances at indicated concentrations. Determining the cell number every 24 h. Exposing cells to the added drugs during the whole experiment, whereas changing the media every 24 h. |
| Concentrations | 3 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 377.41 |
| Formula | C22H20FN3O2 |
| CAS Number | 1129669-05-1 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 10 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 |
|---|
| Phospho-Glycogen Synthase Peptide-2(substrate)
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
TC-G 24 is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. |
| 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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
