Cayman Chemical

An affinity probe which allows TXB2 to be detected through an interaction with the biotin ligand.

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

Eltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase...

A thiophene thiourea derivative that acts as a chaperone to stabilize the retromer complex against thermal denaturation (Kd = ~5 µM); dose-dependently increases the level of retromer proteins, redirects APP from the endosome, and reduces the formation of pathogenic APP in cultured hippocampal...

A synthetic intermediate for pharmaceutical synthesis.

A tyrphostin that is a poor inhibitor of EGFRK (IC₅₀ = 450 μM) and PDGFRK (IC₅₀ > 100 μM) which has been found to inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM; blocks the production of TNF-α, attenuating signaling through NF-κB, the induced...

A lipophilic derivative of ferulic acid, demonstrating increased ability to cross cell membranes; at 10-25 µg/ml, inhibits the release of pro-inflammatory cytokines, blocks the expression of COX-2, and reduces NO generation from LPS-stimulated macrophages.

The precursor of arachidonoyl ethanolamide (AEA), also known as anandamide, an endogenous cannabinoid neurotransmitter that binds to both CB1 and CB2 receptors.

An orally bioavailable antagonist of the androgen receptor (IC₅₀ = 16 nM); at 30 mg/kg/d, suppresses tumor growth in a mouse model of castration-resistant prostate cancer.

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A selective inhibitor of cytohesins, blocking human, mouse, and Drosophila cytohesins with IC50 values of 2.4 to 5.6 µM; prevents cytohesin-dependent insulin signaling in HepG2 cells; produces hepatic insulin resistance in mice.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

A selective inhibitor of matrix metalloproteinase-2 (MMP-2) demonstrating an IC50 value of 12 nM; significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC₅₀ = 50, 4.5, 50, and 2 µM, respectively); suppresses invasive behavior of HT1080 tumor cells grown on matrigel at 50...

Protein MetO is a reversible oxidative modification that occurs by exposure of protein(s) methionine residues to reactive oxygen species (ROS). Methionine oxidation can alter the function(s) of the modified proteins and if not reversed by MetO reductases can be further oxidized to methionine...

A potent, selective ATP-competitive inhibitor of mTOR (IC₅₀ = 0.8 nM); inhibits proliferation of A549 (IC₅₀ = 53 nM) and H838 cells (IC₅₀ = 20 nM) as well as several human tumor xenografts (>65% at 20 mg/kg).

A polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of...

Safingol is the L-threo diastereomer of D-erythro-sphinganine (Item No. 10007945) Both forms of sphinganine inhibit PKC by binding at the regulatory phorbol-binding domain (IC₅₀s = 7 and 24 µM for erythro-sphinganine and safingol, respectively). Safingol also inhibits sphingosine...

A macrolide antibiotic and prodrug of erythromycylamine that has outstanding activity against Campylobacter.

Cayman’s PAF-AH Inhibitor Screening Assay uses 2-thio PAF as a substrate for PAF-AH. Upon hydrolysis of the acetyl thioester bond at the sn-2 position by PAF-AH, free thiols are detected using DTNB also known as Ellman's reagent. Cayman's PAF-AH Inhibitor Screening assay includes human...

A classic macrolide antibiotic produced by strains of Streptomyces that demonstrates antimicrobial activity similar to penicillin and erythromycin.

A competitive inhibitor of human lysosomal β-glucosidase (Ki = 0.016-0.025 µM; IC₅₀ = 0.06 µM) that interacts with the catalytic pocket of β-glucosidase, acting as a chemical chaperone that stabilizes and/or promotes the folding of the enzyme; increases lysosomal...

The primary synthesis of functional vitamin D begins in the skin, where a cholesterol by-product acted upon by UV light forms vitamin D3. Vitamin D3 is carried through the bloodstream, attached to the vitamin D binding protein, to the liver where it is converted to 25-hydroxy vitamin D3 (25(OH)D3)....

A potent CB2 receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.

WS6 is a compound that stimulates the proliferation of pancreatic β cells in rodent and human primary islets (EC_max = 200 and 400 nM, respectively, over four days). It promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse...