1060430-64-9
Chemical Structure
ICL-SIRT078
- CAS No.: 1060430-64-9
- Formula:C28H26N4O2S
- Molecular Weight:482.60
IUPAC Name: 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
InChIKey: UEJBOCXPGHSONP-UHFFFAOYSA-N
SMILES: O=C1C2=C(SC3=C2CCC(C3)NCC4=CC=CN=C4)N=CN1CC5=C(C=CC6=C5C=CC=C6)OC
Biological Activity: ICL-SIRT078 is a substrate-competitive SIRT2 deacylase/deacetylase inhibitor (human SIRT2 IC50 = 0.17-3.96 μM; Ki = 0.62 μM). ICL-SIRT078 acts by binding to the acetyl-lysine pocket and is selective for SIRT2 over other sirtuin isoforms. ICL-SIRT078 induces α-tubulin (α-Tubulin) hyperacetylation and FOXO3a accumulation in breast cancer cells, inhibits cell proliferation, and exerts neuroprotective effects against neuronal cell death in Parkinson's disease[1][2][3].
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ICL-SIRT078 | ICL-SIRT078 is a substrate-competitive SIRT2 deacylase/deacetylase inhibitor (human SIRT2 IC50 = 0.17-3.96 μM; Ki = 0.62 μM). ICL-SIRT078 acts by binding to the acetyl-lysine pocket and is selective for SIRT2 over other sirtuin isoforms. ICL-SIRT078 induces α-tubulin (α-Tubulin) hyperacetylation and FOXO3a accumulation in breast cancer cells, inhibits cell proliferation, and exerts neuroprotective effects against neuronal cell death in Parkinson's disease. | |||||||||||||||||||||
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References
- [1]. Di Fruscia P, et al. The Discovery of a Highly Selective 5, 6, 7, 8‐Tetrahydrobenzo [4, 5] thieno [2, 3‐d] pyrimidin‐4 (3H)‐one SIRT2 Inhibitor that is Neuroprotective in an in vitro Parkinson’s Disease Model. ChemMedChem. 2015 Jan;10(1):69-82.
- [2]. Sundriyal S, et al. Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket. Journal of medicinal chemistry. 2017 Mar 09;60(5):1928-1945.
- [3]. Soni A, et al. Unlocking the Therapeutic Potential of Heterocyclic Molecules as SIRT2 Inhibitors: Advancing Therapeutic Frontiers. Russian Journal of Bioorganic Chemistry. 2026 Aug;52(4):91.
