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| | 1H-Benz[de]isoquinoline-2(3H)-butanamide Basic information |
| | 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 |
| | 1H-Benz[de]isoquinoline-2(3H)-butanamide Usage And Synthesis |
| Uses | Nullscript is a negative control for Scriptaid. Nullscript is a known inactive analog of Scriptaid[1]. Scriptaid is a representative HDAC inhibitor[2]. Nullscript inhibits Cryptosporidium (C. parvum) growth with the IC50 value of 2.1 μM[3]. | | 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. |
| | 1H-Benz[de]isoquinoline-2(3H)-butanamide Preparation Products And Raw materials |
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