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GSK-3 inhibitor 3

Cat. No. M43379
GSK-3 inhibitor 3 Structure
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Biological Activity

GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively.

Chemical Information
Molecular Weight 410.4
Formula C23H15FN6O
CAS Number 2227279-84-5
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Davoud Ghazanfari et al. Bioorg Med Chem. A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism

[2] Sitansu S Nanda et al. Curr Drug Targets. GSK-3 Inhibitors in the Regulation and Control of Colon Carcinoma

[3] Jintao Lin et al. Biochim Biophys Acta Mol Cell Res. GSK-3β in DNA repair, apoptosis, and resistance of chemotherapy, radiotherapy of cancer

[4] Fumi Takahashi-Yanaga. Biochem Pharmacol. Activator or inhibitor? GSK-3 as a new drug target

[5] Richard S Jope. Trends Pharmacol Sci. Lithium and GSK-3: one inhibitor, two inhibitory actions, multiple outcomes

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  Catalog
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Keywords: GSK-3 inhibitor 3 supplier, GSK-3, inhibitors, activators


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