OTS514

• CAT Number: I001292
• CAS Number: 1338540-63-8
• Molecular Formula: C21H20N2O2S
• Molecular Weight: 364.46
• Purity: ≥95%
• Synonyms: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one
• Target: TOPK
• Solubility: 10 mM in DMSO
• Storage: -20°C
• IC50: 2.6 nM
• IUPAC Name: 9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one
• InChI: InChI=1S/C21H20N2O2S/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18/h3-9,12,24H,10,22H2,1-2H3,(H,23,25)/t12-/m0/s1
• InChIKey: OETLNMOJNONWOY-LBPRGKRZSA-N
• SMILES: CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN)O

OTS514（Cat No.:I001292）is a highly potent inhibitor of T-lymphokine-activated killer cell-derived protein kinase (TOPK). TOPK plays a crucial role in cancer cell proliferation and the maintenance of cancer stem cells. By inhibiting TOPK, OTS514 effectively disrupts these processes, offering potential therapeutic benefits against cancer. Additionally, OTS514 downregulates the expression of the oncogenic transcription factor forkhead box protein M1 (FOXM1), further contributing to its anticancer effects.

Reference

[1]. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition ofcytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145.
[2]. Nakamura, Yusuke; et al. Preparation of thieno[2,3-c]quinoline derivatives as PKB inhibitors for treating cancer. From PCT Int. Appl. (2011), WO 2011123419 A1 20111006.