12 products were found matching "Cay11300"!

Methylation of lysine residues in core histones plays a critical role in regulating gene expression. Jumonji domain containing 2D (JMJD2D) catalyzes the demethylation of di- and tri-methylated forms of histone H3 at lysine residue 9 (me 2/3), leading to transcriptional repression and activation, respectively. Like...

The cytochalasins are cell-permeable fungal metabolites that inhibit actin polymerization. This interferes with such diverse processes as cell movement, growth, phagocytosis, degranulation, and secretion. Cytochalasin D is a cell-permeable inhibitor that binds actin filaments, but not actin monomers, to inhibit...

1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become 'analog sensitive' (as), as compared to the wild-type kinase. 1-NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28...

Pterostilbene is a polyketide synthase-derived stilbene originally isolated from P. santalinus that has diverse biological activities. It reduces photooxidative leakage induced by the herbicide acifluorfen in C. sativus cotyledon disks when used at a concentration of 30 µg/ml. Pterostilbene (25 and 50 µM) inhibits...

Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM. While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.Formal Name:...

Anisomycin is a pyrrolidine antibiotic produced by S. griseolus that inhibits protein and DNA synthesis. It activates stress-activated protein kinase, MAP kinase, and other signal transduction pathways. At 30 mg/kg, anisomycin displays immunosuppressive activity superior to that of Cyclosporine A, blocking T cell...

L-Kynurenine is an active metabolite of tryptophan (Cay-29600, Cay-31210). It is formed from tryptophan via tryptophan 2,3-dioxygenase (TDO) or indoleamine 2,3-dioxygenase (IDO). L-Kynurenine binds to the aryl hydrocarbon receptor (AhR, Kd = ~4 µM) and increases the activity of ethoxyresorufin-O-deethylase (EROD) in...

Ascomycin, produced by the fermentation of S. hygroscopicus subsp. ascomyceticus, is an ethyl analog of tacrolimus (FK-506) with potent immunosuppressant properties that prevents T-cell proliferation through initial binding to FK-506-binding protein 12 (FKBP12), an immunophilin that acts as the principal mediator of...

Poly(ADP-ribose) polymerase (PARP) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is activated by DNA damage. Inhibiting its activity has been linked to synthetic lethality and loss of either of the breast cancer susceptibility genes, BRCA1 and...

An anthroquinone derivative that is naturally found in the flower of H. perforatum (St. John's wort) and has antidepressant, antiviral, and anticancer activities. Hypericin inhibits neuronal uptake of serotonin, norepinephrine, dopamine, GABA and L-glutamate, contributing to its antidepressant effects. It exerts...

K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C. However, as this compound does not freely pass through the cell membrane, it is used to inhibit extracellular kinases (ectokinases) of cells in culture. K252b inhibits receptor-mediated...

PGDM-d4 is intended for use as an internal standard for the quantification of PGDM by GC- or LC-MS. PGD2 plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle. PGDM...