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A blood-brain barrier permeable, potent, selective, and reversible antagonist of mGlu7 receptor (IC50 = 3.5 and 2.8 μM for mGlu7a and mGlu7b in CHO cells).
An immunosuppressive and anti-neoplastic agent that inhibits pyrimidine synthesis by blocking the activity of mammalian mitochondrial dihydroorotate dehydrogenase (DHODH; IC50 = 12 nM).
A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310nM vs >40μM; [Mcl-1] & [Bcl-x
A cell-permeable benzophenanthridinone compound that acts as an allosteric and reversible inhibitor of mitochondrial glutaminase activity and represses the growth and invasive activity in glutaminase upregulated fibroblasts and in tumor cells (IC50 ≤ 10μM in NIH3T3 cells stably expressing Dbl, Cdc42-F28L, Rac-F28L or RhoC-F30L mutants and in SKBR3 and MDA-MB231 cancer cel
A cell-permeable compound that increases intralysosomal pH and impairs autophagic degradation process. Suppresses proliferation of human dermal fibroblasts (IC50 = 30 μM).
A cell-permeable, non-toxic, phenylaminopyrimidinyl-acrylamide compound that acts as a highly potent, selective, ATP-site directed, and irreversible inhibitor of Cdk7 (IC50
A cell-permeable, restricted form of CCG-1423 with enhanced potency (IC50 = 4.2 μM vs 16.6 μM for PC-3 cell migration), but reduced off-target toxicity.
A cell-permeable compound that prevents various bacterial toxins from exerting their cytotoxic activity by blocking endosomal trafficking/maturation into acidified late endosomes.