DDO3711

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DDO3711

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2673364-10-6

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-ASK1^T838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。

生物活性

DDO3711, a PP5-recruitingphosphataserecruitment chimeras (PHORCs), is formed by connecting a small molecularapoptosissignal-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-ASK1^T838by 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-ASK1^T838，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-ASK1^T838去磷酸化。DDO3711 浓度依赖性降低 p-JNK 和 p-p38 的水平^[1]。

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-ASK1^T838in 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]。

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-ASK1^T838.

分子量

767.83

Formula

C₄₂H₄₁N₉O₆

CAS 号

2673364-10-6

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.