PROTAC Sirt2 Degrader-1

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Chemical Structure| 2098487-75-1 同义名 : -
CAS号 : 2098487-75-1
货号 : A744244
分子式 : C40H40N10O8S2
纯度 : 95%
分子量 : 852.94
MDL号 : MFCD31813619
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(123.1 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 PROTAC Sirt2 Degrader-12 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-12 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[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.17mL

0.23mL

0.12mL

5.86mL

1.17mL

0.59mL

11.72mL

2.34mL

1.17mL
参考文献

[1]Schiedel M, Herp D, 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.