Serine/threonine-proteine kinase PIM1/PIM2 Inhibitor
     
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Serine/threonine-proteine kinase PIM1/PIM2 Inhibitor

(5Z)-5-[(4-chlorophenyl)methylene]thiazolidine-2,4-dione

Potent inhibitor of PIM-1 with IC50 values of 0.040.03 M. The inhibition of PC3 prostate carcinoma cells proliferation by 21a is 498 M.

Potent inhibitor of PIM-2 with IC50 values of 0.20.1 M. The inhibition of PC3 prostate carcinoma cells proliferation is 498 M.

pim_kinase_inhibitor

OTAVAchemicals Catalogue Number:   0123300047

CAS Registry Number: N/A

Purity: 100%

Ref.: Xia et al. Synthesis and Evaluation of Novel Inhibitors of Pim-1 and Pim-2 Protein Kinases. J. Med. Chem. (2009), 52, 7486.

Abstract: The Pim protein kinases are frequently overexpressed in prostate cancer and certain forms of leukemia and lymphoma. 5-(3-Tri?uoromethylbenzylidene)thiazolidine-2,4-dione (4a) was identi?ed by screening to be a Pim-1 inhibitor and was found to attenuate the autophosphorylation of tagged Pim-1 in intact cells. Although 4a is a competitive inhibitor with respect to ATP, a screen of approximately 50 diverse protein kinases demonstrated that it has high selectivity for Pim kinases. Computational docking of 4a to Pim-1 provided a model for lead optimization, and a series of substituted thiazolidine-2,4-dione congeners was synthesized. The most potent new compounds exhibited IC50s of 13 nM for Pim-1 and 2.3 M for Pim-2. Additional compounds in the series demonstrated selectivities of more than 2500-fold and 400-fold for Pim-1 or Pim-2, respectively, while other congeners were essentially equally potent toward the two isozymes. Overall, these compounds are new Pim kinase inhibitors that may provide leads to novel anticancer agents.

 
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