1H-Benz[de]isoquinoline-2(3H)-butanamide
1H-Benz[de]isoquinoline-2(3H)-butanamide Basic information
- Product Name:
- 1H-Benz[de]isoquinoline-2(3H)-butanamide
- Synonyms:
-
- 1H-Benz[de]isoquinoline-2(3H)-butanamide, N-hydroxy-1,3-dioxo- (9CI)
- 1H-Benz[de]isoquinoline-2(3H)-butanamide, N-hydroxy-1,3-dioxo-
- script
- Nullscript, Inactive analog of scriptaid
- CAS:
- 300816-11-9
- MF:
- C16H14N2O4
- MW:
- 298.29
- Mol File:
- 300816-11-9.mol
1H-Benz[de]isoquinoline-2(3H)-butanamide Chemical Properties
- Melting point:
- 171-172℃
- storage temp.
- −20°C
- solubility
- ≤2mg/ml in DMSO;2mg/ml in dimethyl formamide
- form
- Yellow to off-white solid.
- Sensitive
- Light Sensitive
Safety Information
- Safety Statements
- 22-24/25
1H-Benz[de]isoquinoline-2(3H)-butanamide Usage And Synthesis
Definition
ChEBI: 4-(1,3-dioxo-2-benzo[de]isoquinolinyl)-N-hydroxybutanamide is a member of isoquinolines.
Biological Activity
nullscript is an hdac inhibitor.histone deacetylase inhibitors (hdis) have been used in psychiatry and neurology as mood stabilizers and anti-epileptics, such as valproic acid. recently, hdis are being studied as a mitigator or treatment for neurodegenerative diseases. moreover, there has been an effort to develop hdis for cancer therapy.
in vitro
nullscript, a close analog of scriptaid, was found to be inactive in transcriptional facilitation at corresponding concentrations, which confirmed a minimal requirement for the length of the linker chain expected for this class of hdac inhibitors. in addition, nullscript was not able to induce the p6sbe-luc reporter construct, which was identified from the library using chemfinder by its structural similarity to scriptaid [1].
in vivo
a standard in vivo model of cardiac i/rwe was utilized to examine the in vivo consequences of hdac inhibition in the intact heart. results showed that the treatment with scriptaid led to a nearly identical effect when compared to nullscript, with a 46.8% reduction in infarct size. such results strongly suggested that in murine models, hdacis could reverse the induction of ischemia-induced hdac activity and reduced myocardial infarct size by more than 50% [2].
References
[1] g. h. su, t. a. sohn, b. ryu, et al. a novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. cancer research 60, 3137-3142 (2000).
[2] anne granger et al. histone deacetylase inhibition reduces myocardial ischemia-reperfusion injury in mice. faseb j. 2008 oct; 22(10): 3549–3560.
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1H-Benz[de]isoquinoline-2(3H)-butanamide(300816-11-9)Related Product Information
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- BML-210
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- APICIDIN
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- 1H-Benz[de]isoquinoline-2(3H)-butanamide
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