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SB415286

Cat. No. M3442
SB415286 Structure
Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 420 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

SB 415286 is a potent and selective cell-permeable, ATP-competitive GSK3α inhibitor with an IC50 and a Ki of 78 and 31 nM, respectively. SB 415286 competes with ATP. SB 415286 has minimal activity against 24 other protein kinases (IC50 > 10 μ M). SB 415286 stimulates glycogen synthesis, gene transcription and is neuroprotective. As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway. In L6 myotubes, SB 415286 induced a much greater activation of GS (6.8-fold) . In adipocytes, SB 415286 caused a comparable activation of GS despite a substantial differentiation-linked reduction in GSK3 expression ( approximately 85%) indicating that GSK3 remains an important determinant of GS activation in fat cells. SB 415286 induced expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells.

Protocol
Cell Experiment
Cell lines OPM-2, RPMI-8226, U-266, and INA-6
Preparation method Exposing cells to different concentrations of SB 415286 for 48 or 72 hours in 96-flat well plates. 48 or 72 hours later, [3H]thymidine is added to the cultures (10 μCi/well) for the last 12 hours. Using a top count β-counter to evaluate the [3H]thymidine incorporation by scintillation counting .Assessing apoptosis by annexin V/Propidium Iodide staining or by detection of mitochondrial membrane potential. Evaluating cell death by the analysis of Forward/Side scatter fluorescence changes. Fluorescence Activated Cell Sorting (FACS) analysis is performed .
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation time 48, or 72 hours
Animal Experiment
Animal models Male Wistar rats with acute colitis provoked by trinitrobenzene sulphonic acid (TNBS)
Formulation Dissolved in DMSO
Dosages ~1 mg/kg mg/kg
Administration Administered subcutaneously twice daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 359.72
Formula C16H10ClN3O5
CAS Number 264218-23-7
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB415286 supplier, GSK-3, inhibitors

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