The mitochondrial mitoNEET ligand NL-1 is a mitoNEET inhibitor, which induces a concentration-dependent decrease in cell viability with an IC50 of 47.35 μM and 56.26 μM in REH and REH/Ara-C cells respectively. The docking studies using liver mitochondrial suspensions show the IC50 of NL-1 binding for [3H]-rosiglitazone is 0.9 μM and the Ki for NL-1 site 1 and site 2 was 4.78 and 2.77, respectively.
NL-1 is a mitoNEET inhibitor with antileukemic effect, which induces a concentration-dependent decrease in cell viability of REH and REH/Ara-C, and impaires the migratory ability of leukemic cells irrespective of the chemoattractant used.[2]
NL-1 shows antileukemic activity in an in vivo mouse ALL model.[2]
[1] Geldenhuys WJ, et al. Bioorg Med Chem Lett. 2010 Feb 1;20(3):819-23. [2] Geldenhuys WJ, et al. J Pharmacol Exp Ther. 2019 Jul;370(1):25-34.