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  • DC Chemicals Limited
  • China
  • Product Name: IM-12
  • Price: $600.0/100mg $1000.0/250mg $1800.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1129669-05-1

1129669-05-1 structure
1129669-05-1 structure

Name 3-[2-(4-fluorophenyl)ethylamino]-1-methyl-4-(2-methyl-1H-indol-3-yl)pyrrole-2,5-dione
Synonyms IM-12
3-{[2-(4-Fluorophenyl)ethyl]amino}-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-(4-Fluorophenylethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-(2-(4-fluorophenyl)ethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-[[2-(4-fluorophenyl)ethyl]amino]-1-methyl-4-(2-methyl-1H-indol-3-yl)-
Description IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
Related Catalog
Target

GSK-3β:53 nM (IC50)

In Vitro IM-12 inhibits GSK-3β in ReNcell VM cells, with I50 of 3.8 μM. IM-12 (3 μM) enhances the β-catenin amount, with no further effect at lower or higher concentration. IM-12 (3 μM) also attenuates the proliferation of ReNCell VM cells. IM-12 increases TCF-activity of ReNcell VM[1].
Kinase Assay Cells are lysed in RIPA buffer, supplemented with protease and phosphatase inhibitors and centrifuged for 5 min at 15,000 rpm. Immunoprecipitation of GSK-3β is performed with a specific mouse monoclonal anti GSK-3β [G8] antibody with 5 μg/sample for 2 h at 4°C. The bound protein is precipitated with Protein A/G-Plus agarose-beads (10 μL beads per sample). GSK-3β kinase activity is measured in a reaction mixture containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. 10 μg/sample pGS-2 peptide substrate is used[1].
Cell Assay To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number is determined every 24 h. Cells are exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h[1].
References

[1]. Schmole AC, et al. Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95.

Density 1.3±0.1 g/cm3
Boiling Point 600.2±55.0 °C at 760 mmHg
Molecular Formula C22H20FN3O2
Molecular Weight 377.411
Flash Point 316.8±31.5 °C
Exact Mass 377.153961
PSA 65.20000
LogP 4.02
Appearance yellow-orange
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.675
Storage condition 2-8°C
Water Solubility DMSO: ≥9mg/mL
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
Risk Phrases 22
RIDADR NONH for all modes of transport