Cayman Chemical

A selective DNA-PK inhibitor (IC₅₀ = 14 nM) that increases the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and potentiates the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

A certified reference material that is categorized as a phytocannabinoid; provided as a DEA exempt preparation; intended for research and forensic applications,

A natural O-methylated flavone that reversibly inhibits CYP1A1 and CYP1B1 in human liver microsomes with Ki values of 89 and 16 nM, respectively.

(±)13-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of...

An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC₅₀s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to...

A sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8 sodium channels (IC50 = 8 nM when stimulated at half-maximal inactivation and IC50 = 79 nM at a resting state); dose dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain...

The sirtuins represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs) that catalyze a reaction coupling lysine deacetylation to the formation of nicotinamide and O-acetyl-ADP-ribose. Cayman’s Direct Fluorescent Screening Assay Kits provide a convenient...

A potential metabolite of latanoprost when administered to animals.

Inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37; 5 μM induces the accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.

GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC₅₀ = 390 nM) that does not inhibit GSK-3α. Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and...

A cyclic hexadepsipeptide mycotoxin that has insecticidal activity.

A metabolite of testosterone, produced by CYP3A or by a mutant of CYP107A1.

Immunogen: Synthetic peptide from the C-terminal region of human protein Nrf2 Host: Rabbit Species Reactivity: (+) Human, mouse, and rat Nrf2 Application(s): FC, IF, and WB This C-terminal Nrf2 polyclonal antibody preferentially detects polyubiquitinated Nrf2 at 90 kDa. Nrf2 forms a heterodimer with...

An antioxidative phenolic naturally found in plants, including safflower seed and millet grain; ameliorates atherosclerosis in vivo, reducing lesion area in mice and rabbits.

A dual inhibitor of mPGES-1 and 5-LO (IC₅₀s = 0.4 and 0.2 µM, respectively); reduces the synthesis of PGE2 and LTC4 during zymosan-induced peritonitis in mice, resulting in a significantly diminished inflammatory response.

A metabolite of tryptophan derived from dietary protein that can accumulate to toxic levels in instances of uremia; 250 µM can induce the activation of NF-κB, promoting the expression of both TGF-β1 and Smad3 expression in proximal tubular cells of rats, which is associated with...

Formal Name: 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol CAS Number: 227947-06-0 Synonyms: ?BADGE-HCl-H₂O Molecular Formula: C₂₁H₂₇ClO₅ Formula Weight: 394.9

Binds the ATP-binding site of PKR and blocks autophosphorylation (IC₅₀ = 186-210 nM); protects neuroblastoma cells against cell damage triggered by ER stress; prevents phosphorylation of FADD, preventing apoptosis; reduces phosphorylation of PKR and eIF2α in the brain, enhancing...

An intermediate used in the production of the gastric proton pump inhibitors, omeprazole and esomeprazole; upon degradation it can inhibit CYP2C19 in pooled human liver microsomes (IC₅₀ = 9.7 µM).

A non-alkaloid toxin lignan that blocks tubulin polymerization, thus, inhibiting mitosis; used as a cathartic, purgative, antiviral agent, vesicant, antihelminthic and the starting material for the semi-synthesis of the anti-cancer drugs etoposide, teniposide, and etopophos.

A selective inhibitor of 2-AG biosynthesis via DAGLα (IC₅₀ = 690 nM); 0-12 mg/kg, i.p. in mice dose-dependently inhibits high-fat diet intake and reduces body weight.

A selective, negative allosteric modulator of the mGlu5 (IC50 = 61 nM; Ki = 477 nM); 10 μM results in a near complete blockade of the glutamate response in cortical astrocytes; 30 mg/kg in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant...

An aminoquinoline antimalarial compound; metabolized primarily by CYP2C8 to N-desethylaminodiaquine, which is highly active against P. falciparum and can synergize with amodiaquine; commonly used in combination therapy.

Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings...