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BRD6688

Catalog No.GC13088

HDAC inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

BRD6688 Chemical Structure

Cas No.: 1404562-17-9

Size Price Stock Qty
1mg
$75.00
In stock
5mg
$325.00
In stock
10mg
$433.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 21 nM, 100 nM, and 11.48 μM for HDAC1, 2, and 3, respectively

BRD6688 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.

Reference:
[1] Wagner, F. F.,Zhang, Y.-L.,Fass, D.M., et al. Kinetically selective inhibitors of histone deacetylase 2 (HDAC2) as cognition enhancers. Chem.Sci. 6(1), 804-815 (2015).

Chemical Properties

Cas No. 1404562-17-9 SDF
Chemical Name N-[2-amino-5-(4-pyridinyl)phenyl]-1-pyrrolidinecarboxamide
Canonical SMILES O=C(N1CCCC1)NC2=CC(C3=CC=NC=C3)=CC=C2N
Formula C16H18N4O M.Wt 282.3
Solubility ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.5423 mL 17.7117 mL 35.4233 mL
5 mM 0.7085 mL 3.5423 mL 7.0847 mL
10 mM 0.3542 mL 1.7712 mL 3.5423 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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