Chemistry, like all the natural sciences, Quality Control of 3-Methoxyaniline, begins with the direct observation of nature— in this case, of matter.536-90-3, Name is 3-Methoxyaniline, SMILES is NC1=CC=CC(OC)=C1, belongs to amides-buliding-blocks compound. In a document, author is Yang, Dali, introduce the new discover.
Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors
Histone deacetylase 11 (HDAC11) preferentially removes fatty acid residues from lysine side chains in a peptide or protein environment. Here, we report the development and validation of a continuous fluorescence-based activity assay using an internally quenched TNF alpha-derived peptide derivative as a substrate. The threonine residue in the +1 position was replaced by the quencher amino acid 3′-nitro-L-tyrosine and the fatty acyl moiety substituted by 2-aminobenzoylated 11-aminoundecanoic acid. The resulting peptide substrate enables fluorescence-based direct and continuous readout of HDAC11-mediated amide bond cleavage fully compatible with high-throughput screening formats. The Z’-factor is higher than 0.85 for the 15 mu M substrate concentration, and the signal-to-noise ratio exceeds 150 for 384-well plates. In the absence of NAD(+), this substrate is specific for HDAC 11. Reevaluation of inhibitory data using our novel assay revealed limited potency and selectivity of known HDAC inhibitors, including Elevenostat, a putative HDAC11-specific inhibitor.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 536-90-3. Quality Control of 3-Methoxyaniline.