A cell-permeable inhibitor of all four human AP isoenzymes (Kis =18 and 56 µM for PLAP and NSAP, respectively); also used as a tyrosine phosphatase inhibitor.

A PARP1 inhibitor (IC₅₀ = 450 nM) that displays neuroprotective effects in cultured mouse cortical neurons; also inhibits eosinophilic infiltration into airways of OVA-challenged mice and induces the regression of atherosclerotic plaques in high-fat fed ApoE(-/-) mice.

A cell-permeable analog of FPP that potently inhibits FTase (IC₅₀ = 50-75 nM), preventing farnesylation of Ras; does not inhibit geranylgeranyl transferase at similar concentrations (IC₅₀ > 100 µM); blocks Ras-mediated transformation of NIH 3T3 cells.

A tyrosine kinase inhibitor which acts on EGFR, inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM) and tumor growth in human HN5 tumor xenografts in mice with an ED50 value of 9 mg/kg; drug form of Erlotinib, Tarceva™, is used to treat certain forms of cancer.

A semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.

Artemisinin is a sesquiterpene lactone originally found in Artemisia (wormwood); it is clinically used to treat malaria. Artemisinin exhibits anti-parasitic, antimalarial, cardioprotective, anticancer, and anti-inflammatory activities. This compound inhibits growth of Plasmodium. In animal models…

L-Arginine serves as a common substrate for both NOS and arginase in the cell. NOS catalyzes the oxidation of arginine to citrulline and NO with Nω-hydroxy-L-arginine (NOHA) formed as an intermediate. Arginase, on the other hand, catalyzes the hydrolysis of arginine into urea and L-ornithine.…

An inhibitor of PDGF-BB tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.

A second generation antiepileptic compound used to prevent convulsions in a variety of settings; binds the synaptic vesicle protein SV2A (pIC₅₀ = 5.7), presumably altering vesicle exocytosis; alters the metabolism and turnover of GABA.

An antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO with an IC₅₀ value of 2.2 µM; sensitizes cells to apoptotic stimuli.

An internal standard for the quantification of OEA by GC- or LC-MS.

A selective, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

A selective inhibitor of the mouse carboxylesterases Ces3 and Ces 1f (IC₅₀ = ~0.1 µM); corrects multiple features of metabolic syndrome in obese-diabetic db/db mice and in mice with diet-induced obesity; also inhibits hCES1, the human ortholog of mouse Ces3 (IC₅₀ = ~50 nM).

BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

A microbial metabolite isolated from Streptomyces that is widely used as a selective inhibitor of the 20S proteasome.

11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

Chrysin is a flavone/flavonoid initially found in Passiflora, Oroxylum, and Pleurotis; it is also a byproduct found in propolis. Chrysin exhibits anti-estrogenic, anti-inflammatory, anxiolytic, neuroprotective, cognition enhancing, antioxidative, anti-metastatic, anticancer chemotherapeutic, and…

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

An orally-available, highly selective inhibitor of B-RafV600E (IC₅₀ = 13 nM); less effective against wild type B-Raf (IC₅₀ = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

A monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.

A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

Clodronate is a first-generation non-nitrogen-containing bisphosphonate that is used clinically for its anti-resorptive activity. Clodronate generates formation of a non-hydrolysable ß-? ATP analog that inhibits mitochondrial ADP/ATP translocase and prevents mitochondrial oxygen consumption…

Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues; metabolized by CYP450 enzymes to active metabolites; alters cholesterol…

A nonfixable red fluorescent dye (excitation max: 586 nm; emission max: 605 nm) that can be used as a specific marker for astrocytes and an activity-dependent probe for monitoring regulated exocytosis.

Activates the aryl hydrocarbon receptor (Ki = 5.4 µM), inducing the expression of both detoxifying enzymes, resulting in pyocyanin degradation, and cytokines that facilitate the clearance of bacteria; accelerates neutrophil apoptosis, resulting in resolution of acute inflammation.

An inhibitor of HDAC, including HDAC1 (IC₅₀ = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.

A potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

Anabaenopeptins are cyclopentapeptides found in cyanobacteria such as Microcystis aeruginosa and Oscillatoria agardhii. Anabaenopeptins and other cyanotoxins are typically inhibitors of serine proteases and protein phosphatases (PPs). Anabaenopeptins may also inhibit carboxypeptidases.…

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3