RS6212 

RS6212 is a specific LDH (lactate dehydrogenase) inhibitor with an IC₅₀ value of 12.03 μM . RS6212 inhibits tumor growth and exhibits potent anticancer activity in multiple cancer cell lines^[1].

IC50: 12.03 μM (LDHA)^[1]

Most cancer cells switch metabolism from mitochondrial oxidative phosphorylation to aerobic glycolysis, which is catalyzed by lactate dehydrogenase (LDH). Sonic Hedgehog (SHH) pathway aberrant activation is related to metabolism shifting to glycolysis^[1].
RS6212 (compound 18) (80 μM; 0-72 h) exhibits significantly anti-proliferative activity against cancer cells and (1 μM, 10 μM, 100 μM; 24 h) inhibits Med-MB (SHH MB, medulloblastoma) with an IC₅₀ value of 81 μM^[1].
RS6212 (80 μM; 6 h) decreases LDH activity, glycolytic level, and ECAR (extracellular acidification rate), and (12.03 μM; 6 h) increases NADH level^[1].
RS6212 (0-320 μM; 48 h) inhibits cell growth in HCT116 cells without PARP cleavage nor LC3B–I lipidation^[1].
RS6212 (50 nM and 100 nM; 24 h) increases inhibitory effect against HCT116 cells in combination with 50 nM or 100 nM rotenone. RS6212-Rotenone causes significant cleavage of PARP, thus activates programmed cell death of cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

398.48

C₂₀H₂₂N₄O₃S

2097925-52-3

O=C1C=C(CCC2)C2=NN1CC3CCN(C(C4=CC=CC=C45)=NS5(=O)=O)CC3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Di Magno L, et al. Discovery of novel human lactate dehydrogenase inhibitors: Structure-based virtual screening studies and biological assessment. Eur J Med Chem. 2022 Jul 14. 240:114605.  [Content Brief]