A small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

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 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.

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.

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 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 inhibits NFATc1 and NF-κB activity, inhibits RANKL-induced osteoclastogenesis in vivo.

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 compound that disrupts the Golgi apparatus by inhibiting the activation of ADP-ribosylation factor 1 (ARF1).

OB-1 is a small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitiv

A small-molecule probe that selectively kills cells induced to express mutant RAS.

A small-molecule probe that selectively kills cells induced to express mutant RAS.

BCI is A small-molecule, allosteric inhibitor of DUSP6 (dual-specificity phosphatase 6) with IC50 of 12.3 uM; also inhibits human DUSP1 with IC50 of 11.5 uM; suppresses the ERK-induced activation of Dusp6 and regulates heart size in zebrafish.

A sodium channel inhibitor..

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]