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MedChemExpress - Model GSK-3 inhibitor 3 -2227279-84-5
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. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research[1].MCE products for research use only. We do not sell to patients.
GSK-3 inhibitor 3
MCE China：GSK-3 inhibitor 3
Brand：MedChemExpress (MCE)
Cat. No.HY-154851
CAS：2227279-84-5
Purity：98.72%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
In Vitro：GSK-3 inhibitor 3 (Compound 34) (1 μM) is a highly selective inhibitor of CDK2 and CDK5, with IC50s of 0.22 μM and 1.3 μM for CDK2 and CDK5, respectively[1].
In Vivo：GSK-3 inhibitor 3 (2 mg.kg for i.v., 10 mg/kg for p.o.) shows a T1/2 of 2.5 h (i.v.), and oral bioavailability (F%) of ~100% in male C57BL6 mice [1]. GSK-3 inhibitor 3 (10 mg/kg for p.o.; only once) produces a 33% reduction in pTau396 in Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice [1]. Pharmacokinetic parameters for GSK-3 inhibitor 3(Compound 34) in Mice[1] Route Dose (mg/kg) CL (mL•min-1/kg-1) Vss (L/kg) >Tmax (h) MRT (h) T1/2 (h) AUCtot (μM/h) Cmax (μM) F (%) i.v. 2 23.3 5.4 3.9 2.5 / / / p.o. 10 / / / / 24.3 3.5 ~100
IC50 & Target：GSK-3α 0.35 nM (IC50) GSK-3β 0.25 nM (IC50) CDK2 0.22 μM (IC50) CDK5 1.3 μM (IC50)
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References：
[1]. Hartz RA, et.al. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors. J Med Chem. 2023 Jun 8;66(11):7534-7552. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。