| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
IM-12, an indolylmaleimide analog, is a novel, potent, cell-permeable and selective inhibitor of GSK-3β (glycogen synthase kinase-3β) with potential neuroprotective effects. With an IC50 of 53 nM, it inhibits GSK-3β. An increase in neuronal cells was observed after IM-12 treatment of human neural progenitor cells. By inhibiting the vital enzyme GSK-3beta, IM-12 works through the traditional Wnt signaling pathway. The Wnt pathway participates in cellular functions related to either proliferation or differentiation.
| Targets |
GSK-3β (IC50 = 53 nM)
|
|---|---|
| ln 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. The growth of ReNCell VM cells is also inhibited by IM-12 (3 μM. IM-12 boosts ReNcell VM's TCF-activity[1].
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| ln Vivo |
NA
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| Enzyme Assay |
Protease and phosphatase inhibitors are added after the cells have been lysed in RIPA buffer, and the mixture is centrifuged at 15,000 rpm for 5 min. GSK-3β is immunoprecipitated using a specific mouse monoclonal anti GSK-3β [G8] antibody at a concentration of 5 g/sample for two hours at 4°C. Protein A/G-Plus agarose beads (10 L beads per sample) are used to precipitate the bound protein. 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, and 0.05 mM DTT is used to measure the GSK-3β kinase activity. The pGS-2 peptide substrate (10 g/sample) is employed[1].
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| Cell Assay |
A cell suspension of 50–100 μL is examined using CASY technology and the appropriate program to determine the number of viable cells. ReNcell VM cells are sown at a specific cell number and multiplied for 24 hours. Then the medium is changed to a proliferation medium with the additional ingredients added at the indicated concentrations. Every twenty-four hours, the cell number is determined. The media is changed every 24 hours, but cells are exposed to the added drugs for the duration of the experiment[1].
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| Animal Protocol |
NA;
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| References | |
| Additional Infomation |
3-[2-(4-fluorophenyl)ethylamino]-1-methyl-4-(2-methyl-1H-indol-3-yl)pyrrole-2,5-dione is an organonitrogen compound, an organooxygen compound and a member of maleimides. It is functionally related to an alpha-amino acid.
|
| Molecular Formula |
C22H20FN3O2
|
|---|---|
| Molecular Weight |
377.4115
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| Exact Mass |
377.153
|
| Elemental Analysis |
C, 70.01; H, 5.34; F, 5.03; N, 11.13; O, 8.48
|
| CAS # |
1129669-05-1
|
| Related CAS # |
1129669-05-1
|
| PubChem CID |
25209788
|
| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
600.2±55.0 °C at 760 mmHg
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| Flash Point |
316.8±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
4.02
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
28
|
| Complexity |
656
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])N([H])C1C(N(C([H])([H])[H])C(C=1C1=C(C([H])([H])[H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)=O)=O
|
| InChi Key |
ZKJAZFUFPPSFCO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20FN3O2/c1-13-18(16-5-3-4-6-17(16)25-13)19-20(22(28)26(2)21(19)27)24-12-11-14-7-9-15(23)10-8-14/h3-10,24-25H,11-12H2,1-2H3
|
| Chemical Name |
3-[2-(4-fluorophenyl)ethylamino]-1-methyl-4-(2-methyl-1H-indol-3-yl)pyrrole-2,5-dione
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| Synonyms |
IM-12; IM 12; IM12
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~75 mg/mL (~198.7 mM)
Water: <1 mg/mL Ethanol: ~10 mg/mL (~26.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6496 mL | 13.2482 mL | 26.4964 mL | |
| 5 mM | 0.5299 mL | 2.6496 mL | 5.2993 mL | |
| 10 mM | 0.2650 mL | 1.3248 mL | 2.6496 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02891395 | Completed | Drug: Imatinib Mesylate and Nilotinib |
Graft Versus Host Disease | University Hospital, Lille | December 24, 2012 | Phase 2 |
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