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 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.|
|Incubation time||72 hours|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL
Ethanol 10 mg/mL
Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells.
Schmöle AC, et al. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95. PMID: 20708937.
|Related GSK-3 Products|
SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2.
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively.
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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