BLX-2477 is a potent and selective 15-lipoxygenase-1 (15-LOX-1) inhibitor with an IC50 value of 99 nM. BLX-2477 can inhibit the generation of inflammatory lipid mediators such as 15-hydroxy-eicosatetraenoic acid (15-HETE). BLX-2477 can be used for the research of inflammation and immunology.

Populin (Populoside) is a phenolic glucoside with antioxidant activities. Populin inhibits aldose reductase with an IC50 of 18.55 μM. Populin shows IC50s of 6.76 µM and 1.69 mM in DPPH radical-scavenging and ABTS ·+ radical-scavenging assays. Populin also inhibits D-Sorbitol accumulation.Populin has the potential to be used in the study of diabetic complications.

FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the research of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.

DPC423 free base is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits Kis of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base has demonstrated antithrombotic effects in animal models, and when used in combination with Aspirin, it shows a strong synergistic effect. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis.

MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.

sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).

ZK-813039 is a potent and orally active factor Xa inhibitor. ZK-813039 can prolong prothrombin time. ZK-813039 can be used for the research of cardiovascular disease.

SC-77964 is a potent, selective and orally active matrix metalloprotease (MMP) inhibitor. SC-77964 shows IC50 values < 0.1 nM against MMP-2, MMP-9, and MMP-13. SC-77964 can be used for the research of cancer and inflammation, such as melanoma.

WAY-126299A is an orally active dual-acting 5-1ipoxygenase inhibitor (IC50: 12.2 μM) and leukotriene D4 antagonist (pKB: 6.4). WAY-126299A inhibits antigen-induced leukotriene-dependent bronchoconstriction. WAY-126299A can be used for research of asthma.

BMS-354326 is a tryptase inhibitor with an IC50 of 1.8 nM. BMS-354326 exhibits excellent selectivity against trypsin and most other related serine proteases. BMS-354326 can be used in the research of asthma and inflammatory diseases.

U80215, a dansylated peptide, is a competitive human renin inhibitor with the IC50 of 2.3 μM. U80215 shows excitation and emission maxima at 340 and 530 nm.

S-3483, a Chlorogenic acid derivative, is a reversible, linear competitive glucose-6-phosphatase (Glc-6-Pase) system inhibitor. S-3483 inhibits Glc-6-Pase with a Ki 129 nM in rat liver microsomes. S-3483 specifically inhibits Glc-6-P transporter of renal and liver microsomes.

BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor. BL-122 can increase the level of cGMP in the tissue, promote the expression of nitric oxide (NO), and mediate the relaxation of smooth muscle. BL-122 can be used for the researches of inflammation, immunology and cardiovascular disease, such as asthma and hypertension.

Adenosine-5'-O-diphosphoribose phosphate sodium is a structural analog of NADPH). Adenosine-5'-O-diphosphoribose phosphate sodium is an HMG-CoA reductase inhibitor. Adenosine-5'-O-diphosphoribose phosphate sodium inhibits microsomal HMG-CoA reductase with an apparent Ki value of 550 μM at low thiol concentrations.

2-NH2-PuTP (n2h6ATP) sodium, an ATP analogue, is a competitive pyruvate-stimulated adenylate cyclase inhibitor with a Ki of 1.7 mM.

(GalNAc)3-CPT is a glycoconjugate prodrug that targets the asialoglyco-protein receptor (ASGR) overexpressed on hepatocytes. (GalNAc)3-CPT exhibits significant antitumor activity (IC50 value of 3.07 μM in HepG2 cells) by activating the cGAS-STING pathway and promoting CD8+ T cell infiltration into tumors, thereby inducing tumor cell apoptosis.

Glycerophosphoinositol 4-phosphate (GroPIns-4-P) disodium is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate disodium can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate disodium can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate disodium can be used in research on cancer cell motility and invasiveness.

LW106 is a selective IDO1 inhibitor with an IC50 of 1.57 μM. LW106 has no inhibitory effect on IDO2 and TDO. LW106 inhibits tumor outgrowth by limiting stroma-immune crosstalk and CSC enrichment in the tumor microenvironment. LW106 reduces subpopulation of cancer stem cells (CSCs) in xenografted tumors in which less proliferative/invasive tumor cells and more tumor cells apoptosis. LW106 can be used for the studies of lung cancer and melanoma.

Cs-2d is a selective ceramide synthases Cer1 inhibitor. Cs-2d has potent inhibitory activity toward C. neoformans Cer1, while maintaining a low off-target effect on human hCerS1. Cs-2d has potent antifungal activity with the significant growth inhibition. Cs-2d can be used for invasive fungal infections research.

JNJ-27390467 is a potent, orally active, and selective tryptase inhibitor (human β-tryptase IC50 = 3.6 nM, Ki = 3.7 nM). JNJ-27390467 exhibits excellent selectivity over trypsin of ~5000-fold. JNJ-27390467 shows effects in animal models of airway inflammation. JNJ-27390467 can be used for allergic asthma research.

Guanosine 5'-O-(2-thiodiphosphate) (trisodium) (GDPβS (trisodium)) is a non-hydrolyzable derivative of GDP. Guanosine 5'-O-(2-thiodiphosphate) (trisodium) is an inhibitor of adenylyl caclase (AC) (Ki = 600 nM). Guanosine 5'-O-(2-thiodiphosphate) (trisodium) partially activates AC in the absence of GPT in cerebral cortex membranes of rodent models (EC50 = 400 nM). Guanosine 5'-O-(2-thiodiphosphate) (trisodium) prevents the release of norepinephrine-induced nitric oxide in cardiac ventricular myocytes.

Bis-Cl-ANT-ATP (tetrasodium) is a fluorescent ATP derivative, which undergo spontaneous isomerization. Bis-Cl-ANT-ATP (tetrasodium) selectively inhibits B. pertussis Adenylyl Cyclase (AC) toxin CyaA over mammalian AC1, AC2, and AC5 (Kis = 16, 1,700, 2,400, and 1,600 nM, respectively). Bis-Br-ANT-ATP (tetrasodium) can be used in the study of whooping cough.

Bis-Br-ANT-ATP (tetrasodium) is a fluorescent derivative of adenosine-5’-triphosphate (ATP). Bis-Br-ANT-ATP (tetrasodium) selectively inhibits B. pertussis adenylyl cyclase toxin CyaA (Ki: 12.6 nM). Bis-Br-ANT-ATP (tetrasodium) can be used in Whooping cough research.

DX-9065a (free base) is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a Ki of 41 nM for human FXa. DX-9065a (free base) has low activity against other serine proteases. DX-9065a (free base) has strong anticoagulant actions.

NAPAP is a thrombin inhibitor. It has potent antithrombin activity (Ki: 2.1 nM). NAPAP selectively inhibits thrombin via a rapid binding mechanism, and has weaker inhibitory effects on trypsin, factor Xa, and plasmin. NAPAP can be used in the study of thrombotic diseases (e.g., venous thrombosis, myocardial infarction).

PENAO TFA is the trifluoroacetic acid of PENAO. PENAO is a potent tumour cell mitochondrial toxin. PENAO inactivates tumor cell mitochondria by targeting inner-membrane adenine nucleotide transferase.

NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease.

Davalomilast (Example 100) is an PDE4 inhibitor with anti-inflammatory property. Davalomilast can be studied in research for autoimmune diseases and dermatology research.

(-)-2-Fluorodeoxyarbutin is a fluorinated derivative of the tyrosinase inhibitor deoxyarbutin.

(+)-2-Fluorodeoxyarbutin is a fluorinated derivative of the tyrosinase inhibitor deoxyarbutin.