2. Metabolic Enzyme/Protease PI3K/Akt/mTOR TGF-beta/Smad Cell Cycle/DNA Damage Stem Cell/Wnt Cytoskeleton Epigenetics Apoptosis
  3. FOXO PTEN ROCK Epigenetic Reader Domain PI3K Akt Apoptosis
  4. ROCK2-IN-13

ROCK2-IN-13 是一种选择性 ROCK2 抑制剂。ROCK2-IN-13 通过抑制 ROCK2 激酶活性并降低其核内表达，破坏 ROCK2 与转录共激活因子 p300 和 PGC 1α 的相互作用，进而抑制致癌基因转录。ROCK2-IN-13 能激活 FOXO1 驱动的 PTEN 表达，从而抑制 PI3K/Akt 通路、诱导 G2/M 期细胞周期阻滞并促进细胞凋亡 (apoptosis)。ROCK2-IN-13 由此消除了维持致癌信号传导的 ROCK2 核转录功能，并恢复了抑癌性 PTEN/FOXO1 轴。ROCK2-IN-13 可用于前列腺癌的相关研究。

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ROCK2-IN-13

ROCK2-IN-13 Chemical Structure

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ROCK2-IN-13 相关抗体

Top Publications Citing Use of Products

查看 FOXO 亚型特异性产品:

查看所有亚型
FOXO1 FOXO3

查看 ROCK 亚型特异性产品:

查看所有亚型
ROCK ROCK1 ROCK2

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach[1].

IC50 & Target[1]

ROCKII

 

FOXO1

 

PI3K

 

Akt

 

体外研究
(In Vitro)

ROCK2-IN-13 (compound 25) (30 μM，24 小时) 在人前列腺癌细胞 (PC-3) 中表现出强大的抗增殖活性 (抑制率 84.5%) ，在 PC-3 细胞和 LNCaP 细胞中分别具有 3.7 μM 和 3.9 μM 的 GI50 值，显示出强效且一致的效力，并且对正常细胞的细胞毒性显著较低 (CCD841 细胞的 GI50 为 55.0 μM，HEK-293 细胞的 GI50 为 41.8 μM)[1]。
ROCK2-IN-13 在 PC-3 细胞中降低了高表达的致癌蛋白 FOXA2 (HNF-3β) 以及表达量较低的 FOXO1 的表达[1]。
ROCK2-IN-13 (1-10 μM) 在 PC-3 和 LNCaP 细 胞中诱导 FOXA2 mRNA 浓度依赖性减少和 FOXO1 mRNA 增加，从而导致核内 FOXA2 蛋白减少、FOXO1 核内积累增强、胞质 FOXO1 磷酸化降低，并通过 PTEN 上调最终抑制 PI3K/Akt 轴，进而提高 p27 表达和 Bax/Bcl-2 比值，同时降低细胞周期蛋白 D1 水平[1]。
ROCK2-IN-13 (1-10 μM，24 小时) 在 PC-3 细胞中降低了处于 G1 期和 S 期的细胞比例，并诱导细胞在 G2/M 期显著积累[1]。
ROCK2-IN-13 (1-10 μM) 在 PC-3 细胞中浓度依赖性地诱导细胞凋亡，在 10 μM 浓度下，早期和晚期凋亡细胞比例分别达到 15.7% 和 8.7%[1]。
ROCK2-IN-13 (1-10 μM，48 小时) 在 PC-3 细胞中主要通过激活 PTEN 来抑制 PI3K/Akt 信号通路，而非通过直接抑制 EGFR[1]。
ROCK2-IN-13 (1-10 μM，48 小时) 在 PC-3 细胞中可诱导 PGC-1α mRNA 浓度依赖性增加，显著降低 ROCK1 和 ROCK2 的 mRNA 表达 (对 ROCK2 作用更明显)，减少核内 ROCK2 蛋白水平而保持胞质 ROCK1 不变，通过募集 RNA 聚合酶II 和 PGC-1α 至 FOXO1 启动子区域增强其转录，并通过促进 RNA 聚合酶 II 及关键共调控因子 (ROCK1/2、PGC-1α 和 p300) 与 PTEN 启动子结合来促进 PTEN 转录[1]。

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

ROCK2-IN-13 相关抗体:

Cell Proliferation Assay[1]

Cell Line: PC-3 cells
Concentration: 30 μM
Incubation Time: 24 h
Result: Exhibited the strongt antiproliferative activity achieving inhibition rates exceeding 80%.

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 1, 3, and 10 μM
Incubation Time: 24 h
Result: Reduced the proportions of cells in the G1 and S phases and induced a marked accumulation of cells in the G2/M phase.

Cell Viability Assay[1]

Cell Line: PC-3 cells
Concentration: 1, 3, and 10 μM
Incubation Time: 48 h
Result: Exhibited greater cytotoxicity than Gefitinib (HY-50895) (a selective EGFR inhibitor) and their combined treatment synergistically reduced PC-3 cell viability.
体内研究
(In Vivo)

ROCK2-IN-13 (compound 25) (30 和 50 mg/kg，腹腔注射，每日一次持续 26 天) 在前列腺癌移植瘤模型中能显著抑制肿瘤生长[1]。

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

Animal Model: PC-3 cells (1 × 106, s.c.) induce- BALB/c nude mice (Seven-week-old)[1]
Dosage: 30 and 50 mg/kg
Administration: i.p., daily for 26 days
Result: Significantly and dose-dependently reduced tumor growth in the xenograft model.
Had anti-tumor effect after 26 days of daily administration at 3 mg/kg.
Produced a significantly lower tumor weight than docetaxel.
分子量

372.37

Formula

C18H11F3N4S
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

ROCK2-IN-13 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

ROCK2-IN-13FOXOPTENROCKEpigenetic Reader DomainPI3KAktApoptosisForkhead box OPhosphatase and tensin homologMMAC1Rho-associated protein kinaseRho-associated kinaseRho-kinaseROKPhosphoinositide 3-kinasePKBProtein kinase Bprostate cancerROCK2p300PGC 1αFOXO1PI3K/AktapoptosisPTEN/FOXO1Inhibitorinhibitorinhibit

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