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MSK-1 inhibitor (4-(2-Chlorophenyl)-1H- benzo[d]imidazol-2-amine Hydrobromide)

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. (
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
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