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PROTAC Sirt2 Degrader-1

    级别和纯度:
  • ≥98%
有货

库存信息

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库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
P649475-10mg
10mg 期货 Stock Image
P649475-5mg
5mg 期货 Stock Image

基本描述

别名 PROTAC Sirt2降解剂-1
规格或纯度 ≥98%
英文名称 PROTAC Sirt2 Degrader-1
生化机理 PROTAC Sirt2 降解剂-1 是一种基于 SirReal 的 PROTAC ,可作为 Sirt2 降解剂,由一种高效的同种型选择性 Sirt2 抑制剂、连接体和一种真正的 E3 泛素连接酶 Cereblon 配体组成。PROTAC Sirt2 降解剂-1 的 IC 50 为 0.5
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


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 IC 50 of 0.25 μM for Sirt2 , with no effect on Sirt1/Sirt3 (IC 50 s>100 μM)

In Vitro

PROTAC Sirt2 Degrader-1 (Compound 12; 10 µM, 1-6 hours) induces Sirt2 degradation in HeLa cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HeLa cells Concentration: 10 µM Incubation Time: 1-6 hours Result: Caused Sirt2 degradation, but showed no effect on Sirt1 levels.

Form:Solid

IC50& Target:SIRT2 0.25 μM (IC 50 )

纯度 ≥98%

关联靶点(人)

SIRT2 Tchem NAD 依赖性蛋白去乙酰化酶 sirtuin-2(NAD-dependent protein deacetylase sirtuin-2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SIRT3 Tchem NAD-dependent deacetylase sirtuin 3 (1285 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SIRT2 Tchem NAD-dependent deacetylase sirtuin 2 (3979 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SIRT1 Tchem NAD-dependent deacetylase sirtuin 1 (3505 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SIRT2 Tchem Cereblon/NAD-dependent protein deacetylase sirtuin-2 (35 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name 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 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)
InChi Key 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
Isomeric 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
PubChem CID 135397670
分子量 852.94

化学和物理性质

溶解性 DMSO : ≥ 100 mg/mL (117.24 mM)
分子量 852.900 g/mol
XLogP3 3.200
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 15
可旋转键计数Rotatable Bond Count 18
精确质量Exact Mass 852.247 Da
单同位素质量Monoisotopic Mass 852.247 Da
拓扑极表面积Topological Polar Surface Area 283.000 Ų
重原子数Heavy Atom Count 60
形式电荷Formal Charge 0
复杂度Complexity 1540.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 1
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器