1. PROTAC JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. PROTACs STAT MDM-2/p53
  3. S3D5

S3D5 是一种高效且选择性的 PROTAC 降解剂,靶向 STAT3 (KD = 4.35 μM)。S3D5 可诱导 HepG2 细胞中 STAT3 的降解,而对其他 STAT 蛋白无显著影响。S3D5 具有良好的抗肝癌细胞增殖活性,这可能与其激活 p53 通路有关。S3D5 对 STAT3 蛋白的降解是通过泛素-蛋白酶体系统 (UPS) 介导的。S3D5 可用于肝癌的研究。

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S3D5

S3D5 Chemical Structure

CAS No. : 3033746-21-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S3D5 is a highly efficient and selective PROTAC degrader targeting STAT3 (KD = 4.35 μM). S3D5 induces degradation of STAT3 in HepG2 cells without significant effects on other STAT proteins. S3D5 exhibits good anti-hepatocellular carcinoma cell proliferation activity, which can be explained by activating the p53 pathway. S3D5 degradation of the STAT3 protein is mediated by the ubiquitin–proteasome system (UPS). S3D5 can be used for the study of hepatocellular carcinoma[1].

IC50 & Target

STAT3

4.35 μM (Kd)

体外研究
(In Vitro)

S3D5 (4-20 μM,96 小时) 在 HepG2 细胞中表现出最佳活性,IC50 值为 8.53 μM[1]
S3D5 (0.1-2 μM,24-48 小时) 可诱导 HepG2 细胞中 STAT3 降解 (DC50 = 110 nM) ,且在任何浓度下对 STAT1、STAT2、STAT4、STAT5 和 STAT6 蛋白的影响均很小[1]
S3D5 (2.5-20 μM,96 小时) 以剂量依赖的方式抑制 HepG2 细胞的生长,并在 5 μM 浓度下抑制 293T 细胞的增殖[1]
S3D5 (1-20 μM,14 天) 可显著减少 HepG2 细胞克隆的数量和大小[1]
S3D5 (5 μM,24-72 小时) 可抑制 HepG2 细胞的增殖、迁移和侵袭[1]
S3D5 (0.1-2 μM,48 小时) 剂量依赖性地上调 HepG2 细胞中 p53 和 p21 蛋白水平,同时下调 STAT3 蛋白水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.1 μM, 0.2 μM, 0.5 μM
Incubation Time: 24 h
Result: Induced STAT3 degradation in HepG2 cells.

Cell Proliferation Assay[1]

Cell Line: HepG2 cells
Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 14 days
Result: Led to a significant reduction in both the number and size of HepG2 cell.

Cell Invasion Assay[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Significantly inhibited the invasive ability of HepG2 cells.

Cell Migration Assay [1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Significantly inhibited the migration ability of HepG2 cells.
分子量

956.89

Formula

C41H45F5N6O13S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-179243
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