BRD6688

BRD6688

Catalog Number:
L002373193APE
Mfr. No.:
APE-C5334
Price:
$441
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      • Overview
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          Background

          IC50: 21 nM, 100 nM, and 11.48 μM for HDAC1, 2, and 3, respectivelyBRD6688 is an HDAC inhibitor. A few chromatin modifying enzymes have been implicated in the neurobiology of learning and memory, especially, histone deacetylases (HDACs). HDACs are responsible for catalyzing the posttranslational hydrolysis of acetyl groups from the 3-nitrogen of lysine residues of histone and non-histone proteins.In vitro: BRD6688 was found to demonstrate kinetic selectivity for HDAC2 against HDAC1, an isoform with 95% similarity within the catalytic binding domain. Moreover, BRD6688 could increase histone acetylation (H4K12 and H3K9) in primary mouse neuronal cultures [1].In vivo: Mouse in-vivo study showed that BRD6688 was able to increase the histone acetylation (H4K12 and H3K9) in hippocampal CA1 neurons of CK-p25 mice. Moreove, the increased histone acetylation in brain served as a surrogate pharmacodynamic marker of HDAC engagement and was consistent with previously observed brain pharmacokinetic properties. In addition, BRD6688 rescued the cognitive deficits in CK-p25 mice, a model of neurodegeneration, in a Pavlovian fear conditioning behavioral assay [1].Clinical trial: So far, no clinical study has been conducted.

      • Properties
        • Alternative Name
          N-[2-amino-5-(4-pyridinyl)phenyl]-1-pyrrolidinecarboxamide
          CAS Number
          1404562-17-9
          Molecular Formula
          C16H18N4O
          Molecular Weight
          282.3
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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