2-[(4-chloro-3-nitrophenyl)sulphonyl]anthranilic acid

Biological Activity

CTPI-2 is a selective mitochondrial citrate transporter (SLC25A1) inhibitor th at displays H1299 anti-proliferation activity in a SLC25A1-dependent manner (IC50 <10  μM). When compared with CTPI-1, CTPI-2 exhibits 20-fold higher target affinity (hSLC25A1 KD = 3.5 μM vs. 63.6 μM, respectively) and is ~1000-fold more potent against H1299 sphere-forming capacity. CTPI-2 inhibits mitochondrial respiration and formation of patient NSCLC tumors-derived CSCs spheres in cultures (10-50 μM), as well as suppresses the growth of patent-derived NSCLC exnografts in mice in vivo (28 mg/kg q.o.d. i.p.).