tp2

Thiophene-2 (TP2) is a targeted inhibitor of polyketide synthase 13 (Pks13), specifically designed to disrupt mycolic acid biosynthesis, effectively inducing rapid cell death in mycobacteria. It demonstrates notable anti-tuberculosis activity and exhibits a minimum inhibitory concentration (MIC) value of 1 μM against Mycobacterium tuberculosis.

IETP2 targets low-density lipoprotein receptor-related protein 1 (LRP1) with a KD of 738 nM, making it useful for delivering drugs and imaging agents across the blood-labyrinth barrier (BLB).

TP-2 is a multi-cationic small molecule with a rhomboid shape, serving as an antidote capable of fully neutralizing unfractionated heparin (UFH) and low molecular weight heparin (LMWH). It surpasses protamine in neutralization efficacy and is also biocompatible.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.