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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 |
| Related GSK-3 Products |
|---|
| 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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