Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a Kd value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model.

D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC).

Bz-Pro-Phe-Arg-pNA (Bz-PFR-pNA) hydrochloride is a chromogenic peptide substrate for plasma and glandular Kallikrein, cysteine proteinase (Cruzipain) and Trypsin. Bz-Pro-Phe-Arg-pNA hydrochloride can be used in Factor XII assay.

ORG-20241 is a PDE3/PDE4 dual inhibitor. ORG-20241 has a significant bronchodilator effect and completely prevents allergen induced airway hyperresponsiveness. ORG-20241 can significantly inhibit eosinophil infiltration at high concentrations. ORG-20241 can be used for research on asthma.

BJH-60 is a mitochondrial complex 1 inhibitor. BJH-60 can inhibit mitochondrial oxygen consumption rate with an IC50 of 1.9 μM in A549 cells. BJH-60 shows no PDE inhibitory effect. BJH-60 can be used for the research of cancer, such as breast cancer.

CPA 926 is a prodrug of Esculetin and is orally active. CPA 926 can inhibit the production of MMP in cartilage explants. CPA 926 can be used for the research of inflammation, such as experimental osteoarthritis.

E 3040 is an orally active dual inhibitor of 5-lipoxygenase and thromboxane synthase. E 3040 exhibits anti-inflammatory effect.

OncoACP3 TFA (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3 TFA, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 TFA can be used for prostate cancer research.

OncoACP3 (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 can be used for prostate cancer research.

Idrabiotaparinux sodium is a derivative of Idraparinux synthesized with biotin. Idraparinux is a polymethylated synthetic pentasaccharide known to interact with the antithrombin III and act as anticoagulant.

AMG-126737 is an orally active and highly selective human mast cell tryptase inhibitor with a Ki of 90 nM. AMG-126737 suppresses early/late-phase bronchoconstriction in sheep models. AMG-126737 is promising for research of asthma and allergic diseases.

L 373890 is a selective pyridinone acetamide thrombin inhibitor with a Ki of 0.5 nM. L 373890 shows highly selectivity for thrombin over trypsin (Ki of 570 nM), serine proteases plasmin, tPA, activated protein C, plasma kallikrein and chymotrypsin. L 373890 can be used for thrombosis research.

Vizenpistat is an ENPP1 inhibitor that can be used in the study of cancer.

Potassium perfluorohexanesulfonate is an orally active surfactant found in sera of the general population. Potassium perfluorohexanesulfonate induces adaptive hepatocellular hypertrophy, decreases serum cholesterol and increases alkaline phosphatase in male mice.

LCZ960 is an orally active glucokinase (GK) activator. LCZ960 stimulates GK activity in hepatocytes in vitro and stimulates glucose uptake in vivo through hepatic GK activation. LCZ960 lowers blood glucose in mice with diet-induced obesity (DIO). LCZ960 maintains normoglycemia and improves glucose tolerance in DIO mice and rats. LCZ960 stimulates glycogen synthase flux and increases hepatic glycogen turnover in rats. LCZ960 induces increased hepatic glycogen recycling. LCZ960 can be used to study high-fat diet-induced obesity and type 2 diabetes.

M 16209 is an orally active aldose reductase (AR) inhibitor. M 16209 inhibits partially purified AR from various sources with IC50 values of 0.12, 0.24, 4.5, 1.2 and 9.3 μM for rat lens AR, bovine lens AR, bovine kidney AR, canine lens AR and human placental AR. M 16209 can be used for the research of metabolic disease, such as diabetes.

CK-2289 is an inhibitor of type III cyclic 3'5'-adenosine monophosphate phosphodiesterase (PDE). CK-2289 can inhibit platelet aggregation and decreases mean arterial blood pressure. CK-2289 can be used for the research of cardiovascular disease, such as congestive heart failure.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC50: < 10  nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma.

HW201877 is a potent and orally active 15-prostaglandin dehydrogenase (15-PGDH) inhibitor with an IC50 of 3.6 nM. HW201877 demonstrates robust cellular efficacy in elevating PGE2 levels in A549 cells and exhibits remarkable efficacy in animal models of tissue injury and fibrosis. HW201877 can be used for the study of inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF) and Crohn’s disease (CD).

BMY 20844 is an orally active platelet cAMP phosphodiesterase inhibitor with anti-thrombosis activity. BMY 20844 can elevate cAMP levels and activate protein kinase in platelets. BMY 20844 can be used for the research of cardiovascular disease.

UK-371800 is a highly selective PDE5 inhibitor (IC50 = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein.

P-8977 is a potent dual CO/5-LO inhibitor (IC50 = 0.01 µM). P-8977 can also inhibit cyclooxygenase (CO) (IC50 = 0.53 µM) in 3T3 cells. P-8977 can inhibit ear edema. P-8977 can be used for research on inflammatory skin conditions.

KF-17625 is an orally active bronchodilator. KF-17625 can inhibit bronchoconstriction induced by Carbachol, Histamine, or Leukotriene D4. KF-17625 can inhibit canine tracheal phosphodiesterase (PDE) IV (IC50 = 12 μM) and Concanavalin-A-induced histamine release from rat mast cells (44% inhibition at 10 mM). KF-17625 can be used for the researches of immunology and inflammation.

YM-1 (TFA) is an inhibitor of angiotensin converting enzyme (ACE) that can be obtained from Chrysanthemum boreale Makino.

RBx-7796 (sodium) is a competitive, highly selective, orally active 5-LO (IC50 = 3.5 mM for human 5-LO enzyme) inhibitor. RBx-7796 (sodium) can effectively inhibit 5-LO activity and LTB4 release. RBx-7796 (sodium) can significantly inhibit airway inflammation and bronchial constriction.

PF-3052334 is an orally active, hepatically selective HMG-CoA reductase inhibitor with an IC50 of 1.9 nM. PF-3052334 inhibits cholesterol synthesis, with IC50 values ​​of 0.9 and 730 nM in hepatocytes and muscle cells, respectively. PF-3052334 can be used to study hypercholesterolemia.

AT-1459 is a selective and orally active direct Thrombin inhibitor with a Ki value of 4.9 nM. AT-1459 exhibits excellent antithrombotic activity in both rat models of venous and arterial thrombosis. AT-1459 can be used for research on thrombosis-related diseases.

UK-356202 is a urokinase-type plasminogen activator (uPA) with a Ki value of 0.037 μM. UK-356202 can be used in research related to the topical treatment of chronic ulcerous wounds.

BMS-180431 is an inhibitor of HMG-CoA reductase (IC50: 43 nM).

Bay-y-1015 is an orally active quinoline-based 5-lipoxygenase inhibitor. Bay-y-1015 inhibits LTB4 and LTC4 synthesis. Bay-y-1015 can be used in the research of inflammatory diseases.