Target nature :
MSK-1 (Mitogen- and Stress-Activated Kinase 1)
CAS n° :
not found
Mecanism of action :
inhibition of MSK1
Physico-chemical properties :
upon request
Probe availability :
LIT (Laboratory of Therapeutic Innovation, Illkirch); PCBIS (Illkirch)
Princeps reference :
Bollenbach M, Nemska S, Wagner P, Camelin G, Daubeuf F, Obrecht A, Villa P, Rognan D, Bihel F, Bourguignon JJ, Schmitt M*, N Frossard * (2021) Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel MSK1 inhibitors. An application in an asthma model. Molecules 2021, 26(2), 391. (https://www.mdpi.com/1420-3049/26/2/391#stats_id)
More bibliography :
Nemska S, Daubeuf F, Obrecht A, Israel-Biet D, Stern M, Kessler R, Roux R, Tavakoli A, Villa P, Tissot A, Danger R, Reber L, Durand E, Brouard S, Magnan A, Frossard N and the COLT consortium (2021) Overexpression of the MSK1 kinase in patients with chronic lung allograft dysfunction and its confirmed role in a murine model. Transplantation (doi: 10.1097/TP.0000000000003606)
Other available information on the probe :
White powder, stored at RT
Other information on the target :
MSK1 is a nuclear kinase, taking part in the activation pathway of the pro-inflammatory transcription factor NF-kB and is demonstrating a therapeutic target potential in inflammatory diseases such as asthma, psoriasis and atherosclerosis
Selectivity profile :
not known
In vivo data :
inhibition of allergic asthma in a mouse model (21-day model of eosinophilic airway inflammation induced by ovalbumin)
In vitro data :
inhibition of MSK1 (kinase assay) (IC50 = 1,6 µM)
anti-inflammatory activity: Inhibition of IL-6 production in inflammatory conditions (57% at 30 µM)
Toxicity :
Not toxic:
- in human primary pulmonary fibroblasts in inflammatory conditions (at 30 µM)
- in mice (10 mg/Kg IP)
Chaine SMILES :
Nc3nc2cccc(c1ccccc1Cl)c2[nH]3
Contacter l'auteur de la sonde
