14 products were found matching "Cay13724-%25"!

DC4 crosslinker is a mass spectrometry-cleavable crosslinking reagent (18Å in length) that contains two intrinsic positive charges, which allow cross-linked peptides to fragment into their component peptides by collision-induced dissociation or in-source decay. Initial fragmentation events result in cleavage on...

The aldo-keto reductase (AKR) enzymes constitute a family of related NADPH-dependent oxidoreductases. The 1C subfamily (AKR1C) includes four human hydroxysteroid dehydrogenases, with AKR1C1 being a 20alpha-HSD and the other three being 3alpha-HSDs. AKR1C1 metabolizes progesterone to an inactive progestin,...

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM). AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis...

M 344 is an inhibitor of histone deacetylases (HDACs), inhibiting maize HDAC (IC50 = 100 nM) as well as human HDAC1 (IC50 = 46 nM). It shows a three-fold selectivity for inhibition of HDAC6 over HDAC1 (IC50s = 88 and 249 nM, respectively). M 344 enhances the sensitivity of human squamous carcinoma cells to radiation...

Timolol is a non-selective beta-adrenergic receptor antagonist with log Kd values of -8.27, -9.86, and -6.8 for binding to human beta1-, beta2-, and beta3-adrenoceptors, respectively. It has been reported that only the (S) enantiomer contributes to the beta-blocking effects of racemic timolol, but the weakly active...

Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator. It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the...

Neurodazine induces neuronal differentiation in skeletal muscle cells. In mouse C2C12 myoblasts, neurodazine (2 µM for seven days) upregulated the expression of neuron-specific enolase (NSE), neurofilament 200 (NF200), synapsin, and other neuronal markers. Neurodazine similarly upregulated NSE and NF200 in human...

Ritanserin is a selective antagonist of the serotonin (5-HT) receptor subtype, 5-HT2A. In a radioligand binding assay, ritanserin exhibits high selectivity for 5-HT2A over 5-HT1 receptors (IC50s = 0.9 nM and >1000 nM, respectively). It also demonstrates relatively low affinity for histamine H1, dopamine D2,...

NF 023 is a purinergic P2X1 receptor antagonist (IC50 = 0.21 µM). It is selective for P2X1 over P2X2-4 receptors (IC50s = >50, 28.9 and >100 µM, respectively). It inhibits alpha,beta-methylene ATP-induced vasoconstriction in isolated rabbit saphenous arteries (pA2 = 5.69). NF 023 also inhibits hepatitis C virus...

PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1, IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM). It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM....

Verteporfin is a photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration. It accumulates in these abnormal blood vessels and, when activated by nonthermal red light with a wavelength of 693 nm in the presence of...

Salubrinal is a selective phosphatase inhibitor that prevents dephosphorylation of eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha), protecting PC12 cells from endoplasmic reticulum stress-mediated apoptosis (EC50 = 15 µM). It appears to block the action of protein phosphatase 1 (PP1) on...