12 products were found matching "Cay18110"!

6alpha-Prostaglandin I1 (6alpha-PGI1) is a stable Prostaglandin I2 (PGI2) analog resistant to hydrolysis in aqueous solutions. 6alpha-PGI1 promotes cyclic AMP accumulation in human thyroid slices and cells in a concentration dependent manner. However, it is about 10-fold less potent than the beta-isomer and 100-fold...

N-Desmethylclobazam (CRM) (Cay-18888) is a certified reference material that is structurally categorized as a benzodiazepine. It is a major active metabolite of clobazam, produced primarily by the action of cytochrome P450 isoform 3A4. N-Desmethylclobazam (CRM) positively modulates GABAA receptors (EC50s range from...

Dynorphin A is a heptadecapeptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system, where it is implicated in antinociceptive functions. It acts as an opioid receptor agonist with nanomolar binding affinity to the three major isotypes kappa, µ, and delta (Kis =...

5-Bromouridine 5'-triphosphate (5-BrUTP) is a brominated form of UTP that is used to label RNA during transcription. 5-BrUTP in newly-transcribed RNA is then evaluated immunologically with antibodies. This approach has been used to detect or measure RNA transcription with a variety of imaging and molecular...

Tilmicosin is a macrolide antibiotic. It is active against macrolide-susceptible strains of M. haemolytica, P. multocida, and E. coli (MICs = 4, 4, and 128 µM, respectively), as well as a hyperpermeable strain of E. coli (MIC = 2 µM), and inhibits bacterial protein synthesis (IC50 = 0.36 µM). Tilmicosin (75 mg/kg)...

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. BI-6727 is a dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis. It inhibits proliferation of multiple cancer cell lines with EC50 values ranging...

Inosine-5'-monophosphate (IMP) is a substrate of IMP dehydrogenase (IMPDH), a NAD+-dependent enzyme that generates xanthosine monophosphate. This is a rate-limiting step in the generation of guanosine monophosphate, which is important for DNA, RNA, and glycoprotein synthesis. Inhibitors of IMPDH, including ribavirin...

Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC50 = 0.8 nM) that selectively kills cancer cell...

Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs). RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM). It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively)....

Dynorphin B is a 13-residue opioid peptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system. It acts as a kappa1b-opioid receptor agonist (Ki = 1.1 nM) and has been implicated in antinociceptive functions. Dynorphin B has also been used to prime cardiogenesis in...

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and alpha-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation....

SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage, as well as the...