New inhibitor of human protein kinase ASK1 (MAP3K5, MAPKKK5, MEKK5)
     
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New inhibitor of human protein kinase ASK1 (MAP3K5, MAPKKK5, MEKK5)

2,7- dioxo-2,7 -dihydro-3H-naphtho[1,2,3-de]quinoline-1-carboxylate

New potent and selective inhibitor of ASK1 with IC50 = 3 ?M, Ki=500 nM

Ask1_inh 

OTAVAchemicals Catalogue Number: 7214191049

CAS Registry Number: 175026-96-7

Purity: 95%+ (HPLC)

Ref.: Volynets GP, Chekanov OM, Synyugin AR, Golub AG, Kukharenko OP, Bdzhola VG, Yarmoluk SM. Identification of 3H-Naphtho[1,2,3-de]quinoline-2,7-diones as Inhibitors of Apoptosis Signal-Regulating Kinase 1 (ASK1) J. Med. Chem., 2011, 54 (8), pp 26802686

Abstract: Apoptosis signal-regulating kinase 1 (ASK1) has recently emerged as an attractive therapeutic target for the treatment of cardiac and neurodegenerative disorders. The selective inhibitors of ASK1 may become important compounds for the development of clinical agents. We have identified the ASK1 inhibitor among 3H-naphtho[1,2,3-de]quinoline-2,7-diones using receptor-based virtual screening. In vitro kinase assay revealed that ethyl 2,7-dioxo-2,7-dihydro-3H-naphtho[1,2,3-de]quinoline-1-carboxylate (NQDI-1) inhibited ASK1 with a Ki of 500 nM. The competitive character of inhibition is demonstrated in Lineweaver?Burk plots. In our preliminary selectivity study this compound exhibited strong specific inhibitory activity toward ASK1.


 
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