1H-Benz[de]isoquinoline-2(3H)-butanamide

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.