ICL-SIRT078

a SIRT2 inhibitor with neuroprotective activity; structure in first source

Also Known As:

3-((2-methoxynaphthalen-1-yl)methyl)-7-((pyridin-3-ylmethyl)amino)-5,6,7,8-tetrahydrobenzo(4,5)thieno(2,3-d)pyrimidin-4(3H)-one

Networked: 1 relevant articles (0 outcomes, 0 trials/studies)

1.	Chapman, Kathryn L: 1 article (01/2015)
2.	Dexter, David T: 1 article (01/2015)
3.	Di Fruscia, Paolo: 1 article (01/2015)
4.	Fuchter, Matthew J: 1 article (01/2015)
5.	Harrison, Ian F: 1 article (01/2015)
6.	Jung, Manfred: 1 article (01/2015)
7.	Khongkow, Mattaka: 1 article (01/2015)
8.	Koltsida, Konstantina: 1 article (01/2015)
9.	Lam, Eric W-F: 1 article (01/2015)
10.	Laohasinnarong, Sasiwan: 1 article (01/2015)

1.	Parkinson Disease (Parkinson's Disease) 01/01/2015 - "These results encourage further investigation into the effects of ICL-SIRT078, or an optimised derivative thereof, as a candidate neuroprotective agent in in vivo models of Parkinson's disease." 01/01/2015 - "In concordance with the recent reports that suggest SIRT2 inhibition is a potential strategy for the treatment of Parkinson's disease, we find that compound ICL-SIRT078 has a significant neuroprotective effect in a lactacystin-induced model of Parkinsonian neuronal cell death in the N27 cell line. "
2.	Breast Neoplasms (Breast Cancer) 01/01/2015 - "We report the identification and validation of 3-((2-methoxynaphthalen-1-yl)methyl)-7-((pyridin-3-ylmethyl)amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one (ICL-SIRT078), a substrate-competitive SIRT2 inhibitor with a Ki value of 0.62 ± 0.15 μM and more than 50-fold selectivity against SIRT1, 3 and 5. Treatment of MCF-7 breast cancer cells with ICL-SIRT078 results in hyperacetylation of α-tubulin, an established SIRT2 biomarker, at doses comparable with the biochemical IC50 data, while suppressing MCF-7 proliferation at higher concentrations. "

1.	Sirtuin 2
2.	Sirtuin 1
3.	Neuroprotective Agents
4.	Biomarkers (Surrogate Marker)
5.	Tubulin
6.	lactacystin