OTSSP167 HCl

OTSSP167, also known as OTS167, is an orally available inhibitor of maternal embryonic leucine zipper kinase (MELK) with potential antineoplastic activity. Upon administration, OTS167 binds to MELK, which prevents both MELK phosphorylation and activation; thus inhibiting the phosphorylation of downstream MELK substrates. This may lead to an inhibition of both cell proliferation and survival in MELK-expressing tumor cells.

OTSSP167 (HCLs a highly potent MELK inhibitor with IC50 value of 0.41 nM.

Synonyms:

[GABA-OBzl p-toluene sulfonate, benzyl 4-aminobutyrate tosylate, 4-amino-butyric acid benzyl ester toluene-4-sulfonic acid, H-GABA-OBzl.TosOH, benzyl 4-aminobutanoate p-toluenesulfonic acid salt, Benzyl 4-aminobutanoate 4-methylbenzenesulfonate];

MELK inhibitor Related Products:

OTSSP167

[1]. Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec 21.

[2]. Ji W, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases. PLoS One. 2016 Apr 15;11(4):e0153518.

[3]. Cho YS, et al. The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. Biochem Biophys Res Commun. 2014 Apr 25;447(1):7-11.