NHI-2

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC₅₀ of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC₅₀ = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S and G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppresses tumor growth in murine B78 melanoma tumor model^[1][2]. In Vitro:NHI-2 (50-200 μM, 8 h) inhibits lactate production in HeLa cells^[1].
NHI-2 (12-40 μM, 72 h) inhibits proliferation in B78 cells^[2].
NHI-2 (0.1-100 μM, 48 h) has an EC₅₀ of 32 μM against B78 cells^[2].
NHI-2 (40 μM, 24 h) increases cell apoptosis when combined with either 30 or 60 mM Oxamate (Oxa) (HY-W013032A)^[2].
NHI-2 (40 μM, 24 h) induces cell cycle arrest at S/G2 phases^[2].
NHI-2 affects extracellular acidification rate (ECAR) (12-26 μM, 80 min) and ATP (18 μM, 24 h) production, and has a synergistic effect with Oxa^[2].
NHI-2 acts as NADH competitor, not only affects glycolysis but also impacts mitochondrial metabolism and the NAD+/NADH balance^[2].
In Vivo:NHI-2 (0.9 mg/kg; Intra-tumoral; once daily for 15 days) can suppress tumor volume when combined with immune checkpoint inhibitors (ICIs) in murine B78 melanoma tumor model^[2].