A natural meroterpene that has retinol-like effects on gene expression and properties of the skin; has antioxidant and antibacterial actions; inhibits DNA polymerase and UDP-glucuronosyltransferase 2B7 (IC50 = 41 µM).

A peptide antagonist of PAR2 which blocks activation by trypsin (IC₅₀ = ~50 μM) but not by the synthetic agonist SLIGRL-NH2; does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein; used to study PAR2 action in cells and in animals.

A polysulfated disaccharide that is used as a reference standard for sucralfate.

An inactive analog of U-73122; can be used as a negative control.

A selective, cell permeable inhibitor of MLCK (IC₅₀ = 50 nM).

Blocks mitochondrial complex III; inhibits the activity of the NADH oxidase in certain bacteria.

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

A fluorogenic substrate of palmitoyl-protein thioesterase.

A sulfated bile acid that is used to induce pancreatic acinar cell injury in models of pancreatitis and to study bile acid transport.

A dual inhibitor of DNA-PK and PI3K.

A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

A potent peptide agonist of the GLP-1 receptor (Ki = 136 pM); stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes; protects hippocampal neurons against glutamate-induced apoptosis.

5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1. It is 18 times more potent than PGE2 in activating adenylate cyclase in NCB-20 cell homogenates. 5-trans PGE2 accelerates fibrinolysis by enhancing plasminogen activation mediated by…

ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

A selective inhibitor of human collagenase-3, also known as MMP-13, producing 89% inhibition at 10 µg/ml; used to evaluate the role of MMP-13 in diverse processes.

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

A fluorogenic substrate for human leukocyte and porcine pancreatic elastase; excitation: 355-380 nm; emission 440-460 nm.

A high-affinity fluorescent calcium indicator (Kd = 115 nM for calcium) that is ideal for monitoring low levels of calcium, as are found in resting cells; may be used to buffer intracellular calcium transients.

A potent inhibitor of PORCN (IC₅₀ = 74 pM), completely blocking Wnt secretion into culture media; prevents activation of all evaluated Wnt family members; effective in vivo as well as in vitro; blocks the progression of breast cancer while downregulating Wnt/β-catenin pathway target…

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

A potent, reversible, and cell permeable proteasome inhibitor; a more effective inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing proteasome activities compared to (S)-MG132 (IC₅₀s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL);…

An endogenous agonist for LXRα (EC₅₀ = 325 nM) that can induce the expression of the ABCA1 reverse cholesterol transporter to inhibit the overall absorption of cholesterol; used as a substrate to monitor cholesterol transport or as an endogenous positive control for testing LXR agonists.

17-phenyl trinor PGA2 is a synthetic prostaglandin analog designed for increased half-life and greater potency. There are no published reports of the biological activity of 17-phenyl trinor PGA2 in the literature at this time.

Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC₅₀ = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

Actinomycin D is a polypeptide antibiotic produced from Streptomyces; it exhibits anticancer chemotherapeutic activity but does not display antibacterial benefit. Actinomycin D is clinically used to treat various cancers and is one component of the VAC chemotherapy regimen. Actinomycin D binds DNA,…

A selective antagonist of the dopamine D3 receptor (pKi = 8.0); has high oral bioavailability and enters the central nervous system of the rat.

A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…

A serine proteases inhibitor that is capable of inhibiting trypsin (a digestive system protease; Ki = 15 nM), tryptase (a mast cell protease; Ki = 95.3 pM), and additional proteases in the coagulation cascade including thrombin (Ki = 0.84 μM); 300 mg/kg decreases the total number of eosinophils…