10,12-Tricosadiynoic acid is a highly specific, selective, high-affinity, and orally active inhibitor of acyl-CoA oxidase-1 (ACOX1), it enhances hepatic mitochondrial FAO via the SIRT1-AMPK pathway and PPARα activation. It also reduces liver lipids, ROS accumulation, and insulin resistance, indicating its potential for treating metabolic diseases such as fatty liver, hypertriglyceridemia, and possibly diabetes.

Retaspimycin is a potent inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.

2-Methoxyestrone is a methoxylated catechol estrogen and metabolite of estrone, with a pKa of 10.81.

(2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM.

RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively.

11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.

(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.

Benfluorex hydrochloride (JP-992 hydrochloride) is an activator of nuclear receptor transcription factor HNF4α. It also exhibits lipid-lowering and blood sugar-lowering effects.

Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.