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SB415286

SKU: orb1223168

Description

SB-415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. Pharmacological GSK-3 inhibitors are potential drugs for the treatment of neurodegenerative diseases, cancer and diabetes.

Images & Validation

Key Properties

CAS Number264218-23-7
MW359.72
Purity>98% (HPLC)
FormulaC16H10ClN3O5
SMILESOC1=C(Cl)C=C(NC2=C(C(=O)NC2=O)C2=C(C=CC=C2)[N+]([O-])=O)C=C1
TargetCDK
SolubilityDMSO : ≥ 83.3 mg/mL; 231.57 mM

Bioactivity

In Vitro
SB 415286 (SB-415286) inhibits human GSK-3α with an IC50 of 77.5 nM, and a Ki of 30.75 nM. SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with EC50 of 2.9 μM. SB-415286 stimulates glycogen synthase activity in Chang human liver cells. SB-415286 induces transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells. SB 415286 (SB-415286, 5-44 μM) attenuates B65 cell loss mediated by 1 mM H2O2. SB-415286 (5-44 μM) causes a significant dose-dependent decrease in the fluorescence intensity of DCF, and attenuates B65 ROS production as mediated by 1 mM H2O2. SB-415286 (5-44 μM) also attenuates ROS production in CGN mediated by 1 mM H2O2. SB-415286 (50 μM) induces a substantial suppression of immunoprecipitated GSK3 activity by 97%.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SB-415286 | SB 415286 | SB415286

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    264218-23-7

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    C16H10ClN3O5

    5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
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Protocol Information

SB415286 (orb1223168)

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Available Sizes

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200 mg
500 mg
2 mg
$ 70.00
5 mg
$ 90.00
10 mg
$ 130.00
25 mg
$ 230.00
50 mg
$ 400.00
100 mg
$ 570.00