PROTAC Sirt2 Degrader-1 - CAS 2098487-75-1

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PROTAC Sirt2 Degrader-1 is a PROTAC selectively targeting on Sirt2, consist an isotype-selective Sirt2 inhibitor SirReal as a warhead linked to cereblon ligand thalidomide. PROTAC Sirt2 Degrader-1 led a selective and dose-dependent degradation of Sirt2 at concentration ranging in 0.2-5μM, as well as a time-dependent depletion of Sirt2 at concentration of 10μM post 0.5-2h with a max degradation observed at 2h in HeLa cells. Depletion of Sirt2 by PROTAC Sirt2 Degrader-1 at concentration of 10μM resulted in a more pronounced acetylation of the microtubule network with enhanced process elongation than enzymatic Sirt2 inhibition.

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Molecular Formula C40H40N10O8S2
Molecular Weight 852.94

PROTAC Sirt2 Degrader-1

Synonyms Sirt2-PROTAC-1; Sirt2 PROTAC-1; Sirt2-PROTAC1; Sirt2 PROTAC 1; 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
Solubility Soluble in DMSO
Storage Powder
-20°C
3 years


In solvent
-80°C
6 months



-20°C
1 month
Shipping Room temperature in continental US; may vary elsewhere
InChI Key GRYRXFYWVDWPQY-UHFFFAOYSA-N
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)
Canonical 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

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