PROTAC Sirt2 Degrader-1

• CAT Number: I019547
• CAS Number: 2098487-75-1
• Molecular Formula: C40H40N10O8S2
• Molecular Weight: 852.94
• Purity: ≥95%
• Synonyms: N-[4-[4-[[3-[[2-[[2-(4,6-dimethylpyrimidin-2-yl)sulfanylacetyl]amino]-1,3-thiazol-5-yl]methyl]phenoxy]methyl]triazol-1-yl]butyl]-2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetamide
• InChI: InChI=1S/C40H40N10O8S2/c1-23-15-24(2)44-40(43-23)59-22-34(53)46-39-42-18-28(60-39)17-25-7-5-8-27(16-25)57-20-26-19-49(48-47-26)14-4-3-13-41-33(52)21-58-31-10-6-9-29-35(31)38(56)50(37(29)55)30-11-12-32(51)45-36(30)54/h5-10,15-16,18-19,30H,3-4,11-14,17,20-22H2,1-2H3,(H,41,52)(H,42,46,53)(H,45,51,54)
• InChIKey: GRYRXFYWVDWPQY-UHFFFAOYSA-N
• SMILES: CC1=CC(=NC(=N1)SCC(=O)NC2=NC=C(S2)CC3=CC(=CC=C3)OCC4=CN(N=N4)CCCCNC(=O)COC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM)[1].
PROTAC Sirt2 Degrader-1 (Compound 12; 10 μM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1].

Reference

[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491.
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