OTSSP167 hydrochloride

• CAT Number: I001666
• CAS Number: 1431698-10-0
• Molecular Formula: C25H28Cl2N4O2 • HCl
• Molecular Weight: 523.9
• Purity: ≥95%
• Synonyms: 4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichlorocyclohexa-2,5-dien-1-one;hydrochloride
• Target: MELK
• Solubility: DMSO: ≥ 5.6 mg/mL
• Storage: Store at -20C
• IC50: 0.41 nM
• InChIKey: XDGWHISAOWEFML-BFLZMHAMSA-N

OTSSP167 Hcl is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).IC50 value: 0.41 nMTarget: MELKMELK (maternal embryonic leucine zipper kinase) is a novel therapeutic target for breast cancer and also reported to be highly upregulated in multiple types of human cancer. MELK inhibitor OTSSP167 should be a promising compound possibly to suppress the growth of tumor-initiating cells and be applied for treatment of a wide range of human cancer.

Reference

[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]. Kuner R, et al. The maternal embryonic leucine zipper kinase (MELK) is upregulated in high-grade prostate cancer. J Mol Med (Berl). 2013 Feb;91(2):237-48. doi: 10.1007/s00109-012-0949-1.