| Identification | Back Directory | [Name]
BRD6688 | [CAS]
1404562-17-9 | [Synonyms]
BRD6688
N-[2-Amino-5-(4-pyridinyl)phenyl]-1-pyrrolidinecarboxamide
1-Pyrrolidinecarboxamide, N-[2-amino-5-(4-pyridinyl)phenyl]- | [Molecular Formula]
C16H18N4O | [MDL Number]
MFCD30719257 | [MOL File]
1404562-17-9.mol | [Molecular Weight]
282.34 |
| Chemical Properties | Back Directory | [Boiling point ]
528.2±50.0 °C(Predicted) | [density ]
1.288±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
12.22±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model[1]. | [Biological Activity]
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]. | [IC 50]
21 nm, 100 nm, and 11.48 μm for hdac1, 2, and 3, respectively | [References]
[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). |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
|
| Telephone: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
cjbscvictory
|
| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|