PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.

P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F.

MP 518 is a PDE inhibitor with antihypertensive properties. MP 518 can inhibit cAMP degradation, causing an increase in ICa, and can also antagonize β-adrenergic stimulation, exerting vasodilation.

Desmethyl thiosildenafil is a phosphodiesterase type 5 (PDE5) inhibitor[1].

Desethyl Sildenafil (Sildenafil impurity C) is the impurity of Sildenafil (IC50 of 134.29 μM).

Cipamfylline is a PDE4 inhibitor that can cause PDE4A4 to accumulate in specific areas of the cell through interaction with the ubiquitin scaffolding protein p62. Cipamfylline can be used in the research of atopic dermatitis.

BMS-341400 mesylate (Compound 6) is an orally active and a selective phosphodiesterase 5 (PDE5) inhibitor, with IC50 of 0.3 nM. BMS-341400 mesylate can be used for research of erectile dysfunction.

BC8-15 is a PDE inhibitor with IC50 values of 0.28, 0.22, and 6.46 µM for inhibiting PDE8A, PDE4A, and PDE7A, respectively. BC8-15 can enhance steroidogenesis in mouse Leydig cells.

ASP9831 is an orally active PDE4 inhibitor. ASP9831 inhibits LSP-induced TNF-α production and has anti-inflammatory activity. ASP9831 can be used in fatty liver disease research.

4-Nitrophenyl phenylphosphonate is a substrate for 5'-nucleotide phosphodiesterase.

(±)-BAY-7081 is a racemate of BAY-7081.

(+)-BAY-7081 is an optical isomer of BAY-7081.

SDUY817 is a dual APN/NEP inhibitor, with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. SDUY817 exerts analgesic effects in a concentration- and time-dependent manner, and can be used for research in the field of neuropathic pain disorders.

WY-50295 is an orally active and selective 5-lipoxygenase inhibitor. WY-5029 inhibits LTB4 formation in rat whole blood leukocytes (IC50: 40 μM and oral ED50: 18 mg/kg). WY-50295 can be used in the study of asthma and other leukotriene-dependent diseases.

NCTT-956 is a very effective platelet 12-lipoxygenase (12-LOX) activity-specific inhibitor.

BLX-3887 is a selective 15-lipoxygenase type 1 (15-LO-1) inhibitor with an IC50 of 32 nM. BLX-3887 can be utilized in research related to the 15-LO pathways.

15(S)-HEDE (Compound 8) is an analogue of 15-HEDE-induced acute liver injury and non-alcoholic steatohepatitis (NASH) in mouse models.

Lanisidenib is the inhibitor for isocitrate dehydrogenase that exhibits antineoplastic activity.

Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes.

XW-032 is an apo-IDO1 inhibitor, with an IC50 of 21 nM. XW-032 (TGI = 63%) exhibits potent in vivo anti-tumor efficacy in the CT26 syngeneic mouse model and is expected to be applied in the research of the field of cancer.

L-645164 is a potent inhibitor of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase. L-645164 produces substantial decreases in circulating serum cholesterol concentrations in dogs. L-645164 is promising for research of central nervous system disorders.

4-Hydroxy atorvastatin hemicalcium is a metabolite of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin is metabolized by the cytochrome P450 (CYP) isoform CYP3A4 to form 4-hydroxy atorvastatin.

SID 24785302 is an inhibitor for hexokinase. SID 24785302 inhibits glycolysis, regulates mitochondrial functions, thereby inhibiting the replication of mutant mtDNA.

SE 175 is an organic nitrate compound that acts as an NO donor in vivo following reductive transformation of the nitrate group to nitric oxide. SE 175 stimulates endothelial soluble guanylate cyclase and induces aortic vasorelaxation with an EC50 of 0.20 µM.

AZ513 is a reversible FAAH inhibitor with an IC50s of 551 nM and 27 nM for human FAAH and rat FAAH, respectively. AZ513 inhibits Anandamide.

MeO-Suc-Ala-Ala-Pro-Ala-CMK (MSACK) is an inhibitor of human neutrophil elastase (HNE), with an IC50 of 20.3 μM. MeO-Suc-Ala-Ala-Pro-Ala-CMK can inhibit the hydrolysis of substrates such as elastin in lung tissue by HNE. MeO-Suc-Ala-Ala-Pro-Ala-CMK can be used in the research of related diseases such as chronic obstructive pulmonary disease (COPD).

Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT, IC50 = 0.8 μg/ml) that can be isolated from Streptomyces. Methylspinazarin is selective for COMT over tyrosine hydroxylase.

Verducatib is a cathepsin inhibitor.

TB-9, a Tasiamide B derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.

FGA139 is a cysteine proteases inhibitor with IC50 values of 4.98/3.14 μM for cathepsin B/L. FGA139 reduces LPS-induced NO production in RAW264.7 cells and tumor necrosis factor (TNFα) levels in microglia, and has anti-oxidative stress and anti-inflammatory activities. FGA139 promotes the secretion of neuroprotective metabolites purine and linoleic acid by LPS-stimulated microglia. FGA139 can be used in neuroinflammatory diseases research.