Multi-targeted Kinase Inhibitor containing Liphagal or analog thereof

Siphonodictyal B induces apoptosis in cancer cells

Overview

　The inventors found that Liphagal and its analog Siphonodictyal B inhibited multiple kinase activities in addition to PI3K.　　
　The inhibitors can be used as inhibitors of CDK7, CDK4, CDK6, PIM2, TSSK3, MST4, NEK6, MAP3K, MST3, DDR1, SPHK1, CaMK1, AurA, BRK, CaMK4 and PIM1 kinases.
　Studies using human colorectal cancer cells revealed that Siphonodictyal B induces expression of pro-apoptotic proteins by activation of the P38 MAPK pathway following an increase in intracellular reactive oxygen species, leading to apoptosis.
　In addition, Siphonodictyal B showed anti-tumor effects in a human colorectal cancer cell line tumor-transplanted mouse model.

In vivo antitumor activity of Siphonodictyal B

Related Works

[1] Cancer Medicine 8. 85662-85672(2019)

IP Data

IP No.　 ： WO2018/203564　(JP, EP, US)
Inventor ： SAIJO Ken, ISHIOKA Chikashi, KATOH Tadashi, NARITA Koichi
keyword ： kinaseinhibitor