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COB-187

Chemical Structure : COB-187

CAS No.: 1862177-86-3

COB-187 (COB187)

Catalog No.: PC-72725Not For Human Use, Lab Use Only.

COB-187 (COB187) is a highly potent and selective inhibitor of GSK-3 with IC50 of 22/11 nM against GSK-3α/GSK-3β.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

COB-187 (COB187) is a highly potent and selective inhibitor of GSK-3 with IC50 of 22/11 nM against GSK-3α/GSK-3β.
COB-187 inhibits GSK-3 phosphorylation of β-catenin and, albeit to a lesser extent, glycogen synthase.
COB-187 increases the protein level of β-catenin in RAW 264.7 macrophages.
COB-187 enhances β-catenin localization to the perinuclear and nuclear region in THP-1 macrophage, does not change the β-catenin mRNA level.
COB-187 significantly increases the expression of the Wnt target gene cyclin D1, reduces the phosphorylation of tau in HEK293 cells transfected with tau expression vector.
COB-187 inhibits only 3 kinases at >40% in a panel of 414 kinase assays, more selective relative to Tideglusib.

Physicochemical Properties

M.Wt 302.41
Formula C15H14N2OS2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-hydroxy-4-phenyl-3-(pyridin-4-ylmethyl)thiazolidine-2-thione

References

1. Noori MS, et al. Am J Physiol Cell Physiol. 2019 Dec 1;317(6):C1289-C1303.

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