IM-12 1129669-05-1
Product Description
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Molecular Weight: 377.41 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
In hNPCs, IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and
subsequently increases β-catenin concentration significantly. Through
the activation of canonical Wnt signalling pathway, IM-12 promotes the
neuronal differentiation of human neural progenitor cells.
Cell Assay: [1]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.
Chemical Information
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Contact us if you need more details on IM-12 1129669-05-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 1129669-05-1、1129669-05-1 IM-12. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight: 377.41 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
In hNPCs, IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and
subsequently increases β-catenin concentration significantly. Through
the activation of canonical Wnt signalling pathway, IM-12 promotes the
neuronal differentiation of human neural progenitor cells.
GSK-3β activity assay | IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, compounds are tested in different concentrations diluted in assay buffer 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. Four microlitres of diluted compounds are added to 25 μM pGS-2 peptide substrate, 20 ng recombinant GSK-3β and 1 μM ATP to a total assay volume of 40 μl. The enzymatic reaction is stopped after 30 min of incubation at 30 °C by adding 40 μl KinaseGlo. The luminometric signal is allowed to stabilise for 10 min and the measured with a Glomax® 96 Microplate Luminometer. |
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Cell Assay: [1]
Cell lines | ReNcell VM cells |
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Concentrations | 3 μM |
Incubation Time | 72 hours |
Method | 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 was determined every 24 h. Cells were exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h. |
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
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.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 377.41 |
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Formula | C22H20FN3O2 |
CAS No. | 1129669-05-1 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Solubility (25°C) * | In vitro | DMSO | 75 mg/mL (198.72 mM) |
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Water | <1 mg/mL ( | ||
Ethanol | 10 mg/mL heating (26.49 mM) | ||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name | 3-[[2-(4-fluorophenyl)ethyl]amino]-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on IM-12 1129669-05-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 1129669-05-1、1129669-05-1 IM-12. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : PI3K/Akt/mTOR > GSK-3 Inhibitor
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