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.
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产品名称 | SIRT1 ↓ ↑ | SIRT2 ↓ ↑ | SIRT3 ↓ ↑ | SIRT5 ↓ ↑ | SIRT6 ↓ ↑ | SIRT7 ↓ ↑ | Sirtuin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Selisistat |
++++
SIRT1, IC50: 38 nM |
99%+ | |||||||||||||||||
Resveratrol | ✔ | 98% | |||||||||||||||||
Inauhzin | ✔ | p53 | 99%+ | ||||||||||||||||
Suramin sodium salt |
+++
SirT1, IC50: 297 nM |
++
SirT5, IC50: 22 μM |
99%+ | ||||||||||||||||
Salermide | ✔ | 98% | |||||||||||||||||
Quercetin Dihydrate | ✔ | 95% | |||||||||||||||||
Sirtinol |
+
SIRT1, IC50: 131 μM |
++
SIRT2, IC50: 38 μM |
98%+ | ||||||||||||||||
AGK2 |
+++
SIRT2, IC50: 3.5 μM |
99%+ | |||||||||||||||||
Tenovin-3 | ✔ | p53 | 99%+ | ||||||||||||||||
3-TYP |
++++
SIRT1, IC50: 88 nM |
++++
SIRT2, IC50: 92 nM |
++++
SIRT3, IC50: 16 nM |
95% | |||||||||||||||
Tenovin-6 |
++
SIRT1, IC50: 21 μM |
++
SIRT2, IC50: 10 μM |
+
SIRT3, IC50: 67 μM |
p53 | 99%+ | ||||||||||||||
SirReal2 |
+++
SIRT2, IC50: 140 nM |
99%+ | |||||||||||||||||
Thiomyristoyl |
++++
SIRT2, IC50: 28 nM |
99%+ | |||||||||||||||||
Et-29 | ✔ | 98% | |||||||||||||||||
OSS_128167 |
+
SIRT1, IC50: 1578 μM |
+
SIRT2, IC50: 751 μM |
+
SIRT6, IC50: 89 μM |
98% | |||||||||||||||
SIRT7 inhibitor 97491 |
+++
SIRT7, IC50: 325 nM |
97% | |||||||||||||||||
Nicotinamide | ✔ | 99+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2098487-75-1 |
分子式 | C40H40N10O8S2 |
分子量 | 852.94 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Store in freezer, under -20°C |
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 |
动物实验配方 |