Catalog No.S7159 Synonyms: OTS167
Molecular Weight(MW): 487.42
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
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|Description||OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.|
OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, in which MELK is highly expressed, with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which are novel MELK substrates and are important for stem-cell characteristics and invasiveness. OTSSP167 suppresses mammosphere formation of breast cancer cells through the inhibition of PSMA1 phosphorylation. 
|In vivo||OTSSP167 exhibits significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. In MDA-MB-231 model, intravenous administration of OTSSP167 at 20 mg/kg once every two days results in TGI of 73% The oral administration at 10 mg/kg once a day reveals TGI of 72%. OTSSP167 for multiple cancer types in dose-dependent and MELK-dependent manners with no or a little body-weight loss. |
in vitro kinase assay:MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl2, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-32P]ATP for 30 min at 30 °C. The reaction is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation.
|In vitro||DMSO||0.5 mg/mL warmed (1.02 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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