2. MAPK/ERK Pathway
  3. MAP3K
  4. DDO3711

DDO3711 是一种招募 PP5 的磷酸酶募集嵌合体 (PHORC)，它是通过化学接头将小分子凋亡信号调节激酶 1 (ASK1) 抑制剂连接到 PP5 激活剂而形成的。DDO3711 特异性抑制 ASK1 (IC50 =164.1 nM) 不影响 ASK2 (IC50>20 μM)。DDO3711 通过募集 PP5 使 p-ASK1T838 显着去磷酸化，并显示 ASK1 依赖性抗增殖活性。DDO3711 有抗癌活性，具有用于异常磷酸化癌蛋白研究的潜力。

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DDO3711 Chemical Structure

DDO3711 Chemical Structure

CAS No. : 2673364-10-6

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DDO3711 相关抗体

Top Publications Citing Use of Products

查看 MAP3K 亚型特异性产品:

查看所有亚型
MAP3K5/ASK1 MAP3K7/TAK1 MAP3K8 ASK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research[1].

IC50 & Target[1]

ASK1

164.1 nM (IC50)

ASK2

>20 μM (IC50)

体外研究
(In Vitro)

DDO3711 (15 μM; 24小时) 通过以 PP5 依赖性方式减少 p-ASK1T838，从而对胃癌细胞显示出抗增殖作用。DDO3711 不抑制 GES-1 细胞和 HGC-27 细胞的增殖[1]。
DDO3711 (5 μM; 1-24小时) 以浓度依赖性方式抑制 CDK4/6 和细胞周期蛋白 D1 的表达[1]。
DDO3711 (5-50 μM; 0.5-2 小时) 在体外和细胞中有效地使 p-ASK1T838 去磷酸化。DDO3711 浓度依赖性降低 p-JNK 和 p-p38 的水平[1]。

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

DDO3711 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MKN45 cells
Concentration: 15 μM
Incubation Time: 24 h
Result: Showed strong antiproliferative activity (IC50=0.5 μM).

Cell Cycle Analysis[1]

Cell Line: MKN45 cells
Concentration: 5 μM
Incubation Time: 1-24 h
Result: Inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: MKN45 cells
Concentration: 5, 25, 50 μM
Incubation Time: 0.5-2 h
Result: Could dephosphorylate p-ASK1T838 in a time- and concentration-dependent manner in vitro.
体内研究
(In Vivo)

DDO3711 (20, 40 mg/kg; 腹腔给药; 每天; 持续 21 天)以剂量依赖性方式显着抑制肿瘤生长[1]。

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

Animal Model: Four-week-old BALB/c nude mice with MKN45 cells[1]
Dosage: 20, 40 mg/kg
Administration: IP; daily; for 21 days
Result: Caused significant inhibition of tumor growth in a dose-dependent manner.
Significantly decreased the level of p-ASK1T838.
分子量

767.83

Formula

C42H41N9O6
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

DDO3711 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

DDO37112673364-10-6DDO 3711DDO-3711MAP3KMAP kinase kinase kinase, MEKK, MAPKKKPP5phosphatase recruitment chimerasPHORCsapoptosis signal-regulated kinase 1ASK1ASK2p-ASK1T838 abnormally phosphorylated oncoproteinsMKN45Inhibitorinhibitorinhibit

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