Novel Jak3 inhibitor with high selectivity within the Jak kinase family
     
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Novel Jak3 inhibitor with high selectivity within the Jak kinase family

The Jak3-C interaction has proven to be of great interest due to its role in causing several different types of immunodeficiency disorders. The intense research in this area has important implications including treatment of Severe Combined Immunodeficiency and production of novel immunosuppressant drugs. Inhibitors of Jak3 could play a role in the treatment of autoimmune diseases and the prevention of transplant rejection.

A recent paper at Journal of Medicinal Chemistry describes a potent Jak3 inhibitor with high selectivity within the janus kinase family:

 

CAS Registry Number: 1260181-14-3

3-[5-[4-(2-hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

novel Jak3 inhibitor

 

Thoma et al. Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family. Journal of Medicinal Chemistry (2011), 54, 284-288

 

If you are interested in getting a quote on its custom synthesis or if you have any other biochemicals you would like to get, you could contact our North American Division by phone +1-416-305-9979 or e-mail: This e-mail address is being protected from spambots. You need JavaScript enabled to view it

OTAVAchemicals has extensive experience in the synthesis of highly valuable products for biotech and pharmaceutical applications and it offers a number of INHIBITORS and other biologically active compounds.

Please download our catalog:  OTAVAchemicals_bioactive_small_molecules_JANUARY_2011-01.pdf  for more details.

Please note that we carry in our catalog the following janus kinase family inhibitors:

 

Janex-1 WHI-P131 WP1066
  • selectively inhibits the tyrosine kinase activity of Jak3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases
  • a potent, cell-permeable Jak2 inhibitor; an analogue of the Jak2 inhibitor AG490 that blocks STAT3 and phosphoinositide-3-kinase pathways
CAS RN 202475-60-3

OTAVAchemicals catalog no. 7015070103

 CAS RN 857064-38-1

OTAVAchemicals catalog no. 7070707057

4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol

 

CAS_202475-60-3

(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide

 

CAS_857064-38-1
D'Cruz et al. Targeting mast cells in endometriosis with Janus kinase 3 inhibitor, JANEX-1. American Journal of Reproductive Immunology (2007), 58, 75-97 Verstovsek et al. WP1066, a Novel JAK2 Inhibitor, Suppresses Proliferation and Induces Apoptosis in Erythroid Human Cells Carrying the JAK2 V617F Mutation. Clinical Cancer Research (2008), 14, 788-796
 
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