A small molecule inhibitor of guanine nucleotide exchange factor (GEF) catalytic activity that binds to SOS1 (Kd=14.7 uM) and disrupts GEF-Ras interaction.

A small molecule inhibitor of guanine nucleotide exchange factor (GEF) catalytic activity that binds to SOS1 (Kd=3.4 uM) and disrupts GEF-Ras interaction.

A small molecule inhibitor of HECT-type ubiquitin ligase with IC50 of 6.8/6.3/6.9 uM for Smurf2/Nedd4/WWP1, respectively.

A small molecule inhibitor of HIV-1 entry via the CCR5 coreceptor.

A small molecule inhibitor of polyglutamine (polyQ) aggregation in Huntington's disease neurons.

A small molecule inhibitor of PP2C that activates extensive 3' cleavage at a concentration 50-fold below that required by fluoride or CP..

A small molecule inhibitor of PSD-95/nNOS interaction with IC50 of 31 uM, without inhibiting nNOS catalytic activity.

A small molecule inhibitor of RAD51-mediated homologous recombination.

A small molecule inhibitor of RNA binding protein Lin28 that blocks the Lin28/let-7 interaction, rescues let-7 processing and function in Lin28-expressing cancer cells.

A small molecule inhibitor of RNA-binding protein Hu protein R (HuR) that interferes the HuR homodimerization with Kd of 7 nM.

A small molecule inhibitor of RNA-binding protein Hu protein R (HuR) that interferes the HuR homodimerization with Kd of 90 nM.

A small molecule inhibitor of Staphylococcus aureus sortase with IC50 of 9.3 uM.

A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays.

A small molecule inhibitor of trans-translation that has broad-spectrum antibiotic activity.

A small molecule inhibitor of α4 integrin-dependent cell migration (IC50=0.5 uM, on the motility of Jurkat T cells) that functions by interacting with γ-parvin.

Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect.

Navoximod (GDC-0919; NLG-​919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.

A small molecule iron transport inhibitor that promotes degradation of transferrin receptor-1 in vitro and in vivo, through a nystatin-sensitive lipid raft pathway.

A small molecule ligand for the methyl-lysine binding protein 53BP1 (p53-binding protein 1) with Kd of 22 uM against the 53BP1 tandem tudor domain.

A small molecule mitochondrial protein import blocker that inhibits Erv1 oxidase activity.

A small molecule NADH oxidase ENOX1 inhibitor with IC50 of 10 uM.

PDI inhibitor 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.