10 products were found matching "Cay13282-%25"!

Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM). It binds to 14-alpha sterol demethylase/CYP51 isoform B (AF51B, Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation). It inhibits...

MS-275 is an inhibitor of histone deacetylases (HDACs) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 µM). However, it does not inhibit HDAC8 (IC50 > 100 µM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in...

FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion. In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM). In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that...

Farnesyl alcohol is an isoprenoid that has been found in aromatic plants and has diverse biological activities. It is an agonist of peroxisome proliferator-activator receptor alpha (PPARalpha) and PPARgamma (EC50s = 5.5 and 28 µM, respectively, in a reporter assay using CV-1 cells) and increases the expression of...

L-DOPA is a metabolic precursor of dopamine that is capable of crossing the blood-brain barrier. It is produced from L-tyrosine by tyrosine hydroxylase and metabolized by catechol-O-methyl transferase (COMT). In the brain L-DOPA is converted to dopamine. Formulations containing L-DOPA have been used in stroke...

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Cay-81590). It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCalpha,...

Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases (HDACs). Unlike the HDAC inhibitor suberoylanilide hydroamic acid, which has a fast-on/fast-off HDAC binding rate, pimelic diphenylamide 106 progressively binds HDACs and remains bound after wash-out. As a result, the IC50...

H2S Donor 5a is a stable, cysteine-activated H2S donor. In the presence of excess of cysteine, the concentration of H2S released from this compound reaches a maximum value at 18 min. It does not react with potential cellular nucleophiles such as -OH and -NH2 groups.Formal Name: benzenecarbothioic acid,...

BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFbetaR1 (IC50s = 810 and 1,800 nM, respectively). It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM). BIX02188 inhibits phosphorylation of ERK5 in a...

4-HQN is a heterocyclic building block. It has been used in the synthesis of compounds with antimalarial or antimicrobial activities in vitro.Formal Name: 4(3H)-quinazolinone. CAS Number: 491-36-1. Synonyms: 4-Hydroxyquinazoline. Molecular Formula: C8H6N2O. Formula Weight: 146.1. Purity: >97%. Formulation: (Request...