Cayman Chemical

A serotonin 5-HT1B and 5-HT1D receptor agonist (IC₅₀s = 9.3 and 7.3 nM, respectively) that also has affinity for the 5-HT1F receptor (IC₅₀ = 17.8 nM); constricts human middle meningeal arteries (EC₅₀ = 89.9 nM) and reduces vascular inflammation associated with...

An adenosine analog which shows selective cytotoxicity against both proliferating and non-dividing lymphocytes; inhibits lymphocyte growth with an IC₅₀ value of 45 nM.

Derivative of PGF1α containing a thio-fluorobenzene substituent in the lower side chain; binds to the recombinant human FP receptor with an IC50 value of about 30 nM.

Source: Recombinant N-terminal His-tagged protein expressed in Sf21 cells TIP60 is a member of the MYST family of lysine acetyl transferases. It has been shown to acetylate histones, p53, and the Ataxia Telangiectasia Mutant protein kinase.

Antigen: synthetic phosphopeptide corresponding to amino acid residues surrounding phospho-Ser490,498 of human ATF2 Host: rabbit Cross-reactivity: (+) human ATF2; expected to react with rat ATF2 Applications: WB and IHC (frozen sections) ATF2 binds to both AP-1 and CRE DNA response elements and is a...

PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC₅₀s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively). It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking...

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (K_is = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (K_is = 180 and 300 nM, respectively), as well as several common...

A TNKS1/2 inhibitor.

MEG is a selective iNOS inhibitor and scavenger of peroxynitrite. The EC₅₀ values for inhibition of iNOS (LPS-treated rat lung), eNOS (bovine endothelial), and nNOS (rat brain) are 11.5, 110, and 60 µM, respectively. MEG reacts with peroxynitrite with a second order rate constant of...

Antigen: purified enzyme from mouse macrophages (RAW 264.7 cells) Host: rabbit Cross Reactivity: (+) iNOS from most mammalian species and nNOS (~5%); (−) eNOS Application(s): ICC, IP, and WB NOS catalyzes the biosynthesis of nitric oxide from L-arginine. iNOS is a soluble enzyme found in a...

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain...

A physiologically active metabolite of losartan; a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.

This nuclear receptor assay system utilizes proprietary human cells engineered to provide constitutive, high-level expression of the human thyroid hormone receptor beta (NR1A2), a ligand-dependent transcription factor commonly referred to as TRβ. INDIGO’s reporter cells include the...

A fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme; targets cell walls of pathogens such as S. aureus in a mouse sepsis model of infection.

Host: mouse, clone RIV11 Cross Reactivity: (+) human CD8 Application(s): FC, ICC, and IHC (frozen sections)

PGE2-EA is an analog of PGE2 with improved water solubility and stability. PGE2-EA acts as an agonist with all four known EP receptor subtypes, but with an affinity that is significantly reduced compared to PGE2. PGE2 ethanolamide is produced by HCA-7 cells treated with AEA. The physiologic...

A major phase I metabolite of tamoxifen, a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium; has at least a 100-fold higher affinity for estrogen receptors than tamoxifen.

An inactive control for the selective PAD4 inhibitors, GSK484 and GSK199 (IC₅₀s >100 µM).

A metabolite of dapsone, an anti-inflammatory and antibacterial compound that is widely used in the treatment of leprosy, malaria, acne, and various immune disorders.

An NSAID that reduces edema in certain types of acute inflammation in animal models; a poor inhibitor of prostaglandin synthesis, but, like other NSAIDs, it inhibits OAT1 (Ki = 32 µM).

A water-soluble azo compound used extensively as a free radical generator.

The phosphate ester (and water-soluble prodrug) of AEA (Item No. 90050); acts with equal potency as AEA in the treatment of C6 glioma cells in vivo; 5-fold less potent than AEA as an agonist of isolated rat brain CB1 receptors (Ki = 200 nM); also a structural variant of LPA.

A ratiometric mass spectrometry probe that can be used for assessing mitochondrial matrix H₂O₂ concentration in vivo.