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.

A small molecule positive allosteric modulator of both proton and vanilloid activation of TRPV1 (EC50=21.3 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.

A small molecule ROS inducer that induces rapid cell death in cancer cells, induces reactive oxygen species via cellular glutathione depletion.

A small molecule sigma receptor ligand with Ki of 96 and 70 nM for sigma 1 and sigma 2, respectively.

A small molecule Skp2 E3 ligase inhibitor that prevents Skp2-Skp1 interaction and Skp2 SCF E3 ligase activity in vitro.

A small molecule TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors.

A small molecule that disrupt 14-3-3 dimers at low micromolar concentrations and induce rapid down-regulation of Raf-MAPK and PI3K-Akt signaling in Jurkat cells.

A small molecule that inhibits NFATc1 and NF-κB activity, inhibits RANKL-induced osteoclastogenesis in vivo.

A small molecule that inhibits N-myristoyltransferase (NMT1) with IC50 of 8.7 uM, 10-fold enhanced inhibitory potency than LCL4.

A small molecule that inhibits the activities of E. coli DNA polymerase I and calf thymus DNA polymerase alpha..

NSC243928(NSC-243928 ) is a small molecule that potently inhibit ovarian cancer stem-like cells (CSC) growth with GI50 of 0.83 uM, which os consistent with cell death/apoptosis..

A small molecule that promotes differentiation of iPS-derived hepatocytes.

A small molecule that rapidly downregulates abscisic acid (ABA)-dependent gene expression (IC50=3 and 1.5 uM for RD29B and RAB18 promoters), also inhibits ABA-induced stomatal closure.

A small molecule that specifically inhibits the clathrin adaptor complex AP-1-dependent traffic, does not significantly affect other pathways through the trans-Golgi network (TGN).

A small molecule with activity against drug-resistant and persistent tuberculosis.

A small molecule, direct STAT3 inhibitor that inhibits the IL-6-induced SEAP expression with IC50 of 200-500 nM, blocks the binding of the activated STAT3 dimers to DNA.