10 products were found matching "Cay16715"!

Celiprolol is a beta1 adrenergic receptor antagonist and a beta2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 µM in vitro. At 1-10 mg/kg/h, celiprolol can reduce myocardial infarct size and increase nitric oxide (NO) production in a rabbit model...

Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFalpha component (a RUNX protein) and an enhancer of binding, CBFbeta. CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias. CBFbeta inhibitor is a small molecule that binds to CBFbeta...

gamma-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and beta-amyloid precursor protein (APP), within the transmembrane domain. Avagacestat is a potent, orally bioavailable inhibitor of gamma-secretase that more potently inhibits the cleavage of APP to...

Carbonic anhydrases are zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide to form bicarbonate ion plus a proton. Carbonic anhydrases IX (CAIX) and CAXII are hypoxia and HIF-1-inducible proteins located in cellular transmembranes that regulate intra- and extracellular pH under hypoxic...

Amastatin is a slow, tight binding, competitive aminopeptidase (AP) inhibitor, first described as an inhibitor of human serum AP-A (glutamyl AP, IC50 = 0.54 µg/ml) but not of AP-B (arginine AP). It also inhibits AP-N (AP-M, alanyl AP, Ki = 20-200 nM), leucyl-cystinyl AP (Ki = 20-220 nM), and endoplasmic reticulum AP...

CZC-8004 is an aminopyrimidine that binds a range of tyrosine kinases, including ABL, BTK, FAK, FER, JAK1, SRC, SYK, TEC, TNK1, TYK2, and YES. It inhibits these kinases at low micromolar concentrations and can be immobilized to capture and purify these enzymes.Formal Name:...

Semagacestat is a potent inhibitor of gamma-secretase that blocks the production of Abeta38, Abeta40, and Abeta42 with IC50 values of 12.0, 12.1, and 10.9 nM, respectively. It also blocks Notch signaling (IC50 = 14.1 nM). Semagacestat modulates gamma-secretase activity in vivo, altering Abeta levels in brain,...

Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family. A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer. NVP-BSK805 is a...

Accumulation of the beta-amyloid (Abeta) peptide in the brain is implicated as the primary cause of neurodegeneration and progression of Alzheimer's disease. Abeta is derived from sequential proteolytic cleavage of the amyloid precursor protein (APP) by beta-secretase (BACE) and gamma-secretase. LY2811376 is a...

Nucleophosmin is a nucleolar phosphoprotein involved in cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, centrosome duplication, and molecular chaperoning. Its activity is dependent on oligomerization at its N-terminal domain, and it is abundantly expressed...