LDHA-IN-1

LDHA-IN-1 is a selective, competitive LDH-A inhibitor, with K_i values of 8.9 μM (NADH assay) and 4.7 μM (Pyruvate assay) against hLDH-A. LDHA-IN-1 inhibits cancer cell proliferation under hypoxic conditions. LDHA-IN-1 can be used in the research of ovarian cancer, colorectal cancer, mesothelioma and pancreatic cancer^[1]. In Vitro:LDHA-IN-1 (Compound 1j) is a potent inhibitor that acts on purified hLDH-A, with a K_i value of 8.9 μM against NADH and 4.7 μM against pyruvate, while it exhibits only weak inhibitory activity against LDH-B^[1].
LDHA-IN-1 (500 μM; 6-12 h) potently inhibits the conversion of glucose to lactate in HeLa cervical cancer cells, reducing the lactate/glucose peak ratio to <0.01 after 12 h of incubation^[1].
LDHA-IN-1 (1-100 μM; 48 h) inhibits the proliferation of various cancer cell lines and primary pancreatic cancer cultures under normoxic conditions, with an IC₅₀ range of 10.8 μM to 90.2 μM, and shows no cytotoxicity towards immortalized normal cell lines at concentrations up to 100 μM^[1].
LDHA-IN-1 (1-100 μM; 48 h) shows significantly enhanced inhibitory potency against primary pancreatic cancer cells LPC006 under hypoxic conditions, with an IC₅₀ of 0.90 μM^[1].