DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration ( IC 50 =1.6 μM, K i =1.23 μM). DS44960156 specifically binds to the active site of MTHFD2 , disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD + /NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers.
Products | Products > Disease Areas > Cancer | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Disease Areas > CNS Neoplasm | Products > Disease Areas > Glioma | Products > Disease Areas > Glioblastoma | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Neurological Disease | Products > Signaling Pathways > Methylenetetrahydrofolate Dehydrogenase (MTHFD)
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