Cayman Chemical

A potent anti-tumor agent used as a selective and irreversible inhibitor of the 20S proteasome; inhibits proteasome activity in cell growth assays (IC50 = 4 nM) and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells (IC50s =...

A broad-spectrum benzimidazole anthelmintic that is active against gastrointestinal parasites (IC₅₀ = 0.30 µM against Giardia in vitro) by targeting tubulin; activates HIF-1α, abrogating oxidative stress-induced death in primary neurons in vitro.

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

An orally bioavailable CFTR potentiator that improves chloride transport; increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D mutation by ~4-fold (EC₅₀ = 100 nM); increases chloride secretion in cultured human CF bronchial epithelial cells...

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type...

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing...

An internal standard for the quantification of PGA2 by GC- or LC-MS.

Source: recombinant N-terminal hexahistidine-tagged protein expressed in E. coli Mr: 19.1 kDa

A selective inhibitor of TAF1 bromodomain 2 (IC₅₀ = 2.1 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

A natural quinoid diterpene that, at 10-20 µM, stimulates AMPK in C2C12 myotubes and activates p38 MAPK in DU145 cells; inhibits SHP2 in vitro (IC₅₀ = 22.5 µM) and, at 4-8 µM, blocks phosphorylation of STAT3 in MC-3 cells; has a variety of anti-cancer actions.

16-phenoxy tetranor PGE2 is the free acid form of sulprostone formed by the hydrolysis of the methylsulfonamide bond. 16-phenoxy tetranor PGE2 is a minor metabolite of sulprostone found in human plasma after parenteral administration of the drug.

A potent inducer of chondrocyte differentiation from human mesenchymal stem cells (EC50 = 100 nM); promotes cartilage repair in a mouse model of osteoarthritis and protects against cytokine-induced damage in osteoarthritic bovine articular chondrocytes in vitro.

An antibiotic that inhibits DOXP reductoisomerase, a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis; against both Gram-negative and Gram-positive bacteria and the human malarial parasite P. falciparum (IC₅₀ = 290-370 nM).

LTC4 is the parent cysLTs produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and...

An inhibitor of PKA, PKC, and PKG (IC₅₀s = 8, 12, and 4 µM, respectively); less effectively blocks the activity of MLCK (IC₅₀ = 240 µM).

A selective inhibitor of DAGLβ (IC₅₀ = 42 nM); disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.

A structural homolog of rosiglitazone that binds PPARγ with about 1/10 the affinity of rosiglitazone yet is a more potent antidiabetic agent in whole animal experiments than rosiglitazone (ED₅₀s = 2.7 mg/kg and 7.1 mg/kg, respectively).

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC₅₀ = 460 nM).

The COX (human) Inhibitor Screening Assay Kit directly measures PGF2α by SnCl2 reduction of COX-derived PGH2 produced in the COX reaction. The prostanoid product is quantified via ELISA using a broadly specific antiserum that binds to all the major prostaglandin compounds. This assay includes...

A potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.

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 synthetic macamide that irreversibly inhibits FAAH with an IC₅₀ value of 0.153 µM.

A minor CYP450 metabolite of arachidonic acid that stimulates vasodilation of rabbit kidney.

A selective and reversible inhibitor of MAO-B (IC50s = 0.48 and 1.5 μM measured in platelets of human subjects ages 19-36 and 60-78, respectively) that is structurally similar to phenyethylamine; evaluated in clinical trials for possible neuroprotectiove actions in the treatment of...