pi-103

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2 3 3 15 30 23 nM for p110α β δ γ, mTOR, and DNA-PK).

PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].

RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug featuring an autocyclized portion connected to the pan-PI3K inhibitor (PI-103). In MDA-MB-361 and MDA-MB-231 cells, Doxorubicin and RIDR-PI-103 exhibited synergistic inhibition of cancer cell proliferation.

PIK-inhibitors (MDK34597) is a pan PI3K inhibitors, an analog of PI-103.