lipid a 4'kinase

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and a potent chemosensitizer that enhances the number of DNA double-strand breaks induced by Doxorubicin. It serves as an effective multidrug resistance (MDR) inhibitor, demonstrating inhibitory activity against P-glycoprotein (P-gp) mediated drug efflux. Multi-target kinase inhibitor 4 can be encapsulated in PEG-coated lipid nanoparticles.

TMX-4102 is a highly selective binder of phosphatidylinositol 5-phosphate 4-kinase Type II gamma (PIP4K2C). It demonstrates binding activity to PIP4K2C with a dissociation constant (KD) of 0.45 nM, and does not significantly affect other lipid and non-lipid kinases. By specifically binding to PIP4K2C, TMX-4102 regulates its scaffold function rather than its enzymatic activity. TMX-4102 serves as a tool molecule for studying the biological functions and potential therapeutic value of PIP4K2C.

Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).