Cayman Chemical

An LDH inhibitor (Kis = 5.46 and 15.06 µM, for the A and B isoforms, respectively) that prevents proliferation of many different cancer cells by blocking glycolysis and ATP production.

A potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki = 0.38 nM); inhibits proliferation in a panel of cancer cell lines that overexpress CK2 and prevents tumor growth of breast and pancreatic cancer cell xenografts in mice.

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

A small molecule that induces autophagy and selectively causes lethality in renal cell carcinoma cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM).

An inhibitor of EHMT2, also known as G9a, decreasing di- and trimethylation on lysine 9 of histone 3 (EC50 = 5 µM); induces senescence in the pancreatic cancer cell line PANC-1 without initiating apoptosis.

A selective inhibitor of PDE3A and PDE3B (IC₅₀s = 27 and 50 nM, respectively); inhibits thrombin-induced platelet aggregation (IC₅₀ = 1.1 μM).

A quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC₅₀s = 105, 34, and 29 nM in vitro); inhibits anchorage-dependent and -independent growth, induces cell cycle arrest, and causes apoptosis in colon and melanoma cell lines carrying B-RafV600E...

An inhibitor of NADPH-oxidase complex assembly that at 300 μM is effective in preventing the production of superoxide in human white blood cells or neutrophilic granulocytes; widely used as an inhibitor of NADPH oxidase activity in the treatment of various inflammatory diseases.

Used to ablate larval melanocytes in zebrafish in order to study melanocyte regeneration.

The CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium...

A potent MEK inhibitor that suppresses phosphorylation of ERK in murine colon 26 tumors with an IC50 value of 0.33 nM; suppression of ERK activation with 1 µM PD 0325901 combined with 3 µM CHIR99021 (a glycogen synthase kinase-3 inhibitor) prevents cell differentiation and sustains self...

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...

Phenolic compounds, particularly flavonoids, from plant sources have long been observed to have antioxidant activity with potential benefits for human health. EGCG is a principle phenolic antioxidant found in a variety of plants, including green and black tea. EGCG inhibits cellular oxidation of low...

A sulfide-like inhibitor of PDE7 (IC₅₀ = 2.1 µM).

A natural product with anti-inflammatory, anti-tumor, and neuroprotective effects; inhibits GSK-3 (IC₅₀ = 2.5 μM) and Cdk1 and 5 (IC₅₀ = 10 μM for both isoforms).

PGF1α is the putative metabolite of DGLA via the COX pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10−11 M. PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the...

FeTMPyP is a synthetic porphyrin complexed with iron, which acts as a peroxynitrite decomposition catalyst. The rate constant for decomposition of peroxynitrite by FeTMPyP is 2.2 x 106 M−1s−1 with a turnover number of 360 ± 170 s−1. The predominant product (>90%) of this...

(±)5-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid. It contains equal amounts of 5(S)-HETE and 5(R)-HETE. (±)5-HETE induces the aggregation of isolated neutrophils with an IC₅₀ value of 200 nM.

LTB4 dimethyl amide is a moderate inhibitor of LTB4-induced degranulation of human neutrophils (Ki = 130 nM) and lysozyme release from rat PMNL. LTB4 dimethyl amide appears to be an antagonist of the LTB4 receptor on guinea pig lung membranes.

Cayman’s STAT-8-isoprostane ELISA is a competitive assay that permits the rapid measurement of 8-iso PGF2α from biological samples, requiring only 1 hour incubation and development times for each step. This assay format is similar to that employed in Cayman’s original 8-isoprostane...

A selective antagonist of GABAB receptors (IC50 = 43 µM); active at presynaptic, but not postsynaptic, receptors.

A metabolite of the nucleoside reverse transcriptase inhibitor, zidovudine, formed by direct conjugation by UGT2B7.

A selective inhibitor of JAK3 with an IC50 value of 78 µM that does not affect the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM); induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous...

The main saponin constituent of C. asiatica that has been shown to improve wound healing including increasing collagen synthesis and elevating antioxidant levels in various normal and diabetic wound models.