2. Cell Cycle/DNA Damage Stem Cell/Wnt Cytoskeleton TGF-beta/Smad JAK/STAT Signaling
  3. ROCK STAT
  4. ROCK2-IN-10

ROCK2-IN-10 是一种强效且具有选择性的 ROCK2 抑制剂 (IC50 = 0.020 μM)，其对 ROCK2 的选择性是亚型 ROCK1 的 41 倍。ROCK2-IN-10 通过破坏细胞骨架来抑制肿瘤转移，该机制不依赖于对细胞增殖的抑制。ROCK2-IN-10 对癌细胞转移的抑制效力与其对 STAT3 磷酸化的抑制密切相关。ROCK2-IN-10 可用于乳腺癌转移的相关研究。

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ROCK2-IN-10

ROCK2-IN-10 Chemical Structure

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ROCK2-IN-10 相关抗体

Top Publications Citing Use of Products

查看 ROCK 亚型特异性产品:

查看所有亚型
ROCK ROCK1 ROCK2

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research[1].

IC50 & Target[1]

ROCK2

0.020 μM (IC50)

ROCK1

0.821 μM (IC50)

体外研究
(In Vitro)

ROCK2-IN-10 (compound S9) 对于 ROCK2 的有效抑制是由于其乙酰氨基侧链与 ROCK2 中 Asp218 和 Asn219 形成的氢键相互作用[1]。
ROCK2-IN-10 (5 μM，24 小时) 可破坏 MDA-MB-231 细胞的整体形态，导致细胞伪足变钝，且沿细胞轮廓分布的 F-肌动蛋白应力纤维出现断裂[1]。
ROCK2-IN-10 (2.5-5 μM，0-48 小时) 在 MDA-MB-231 细胞中表现出强效且剂量依赖性的细胞迁移抑制作用，并且在 24 小时和 48 小时均显示出优于 Belumosudil (HY-15307) 的功效[1]。
ROCK2-IN-10 (2.5-5 μM，24 小时) 以剂量依赖性方式下调 STAT3 的磷酸化水平，从而对 MDA-MB-231 细胞表现出良好的抗转移作用[1]。
ROCK2-IN-10 (72 小时) 在 MDA-MB-231 细胞中表现出极低的细胞毒性，其 IC50 为 12.77 μM[1]。

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

ROCK2-IN-10 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 and 5 μM
Incubation Time: 24 h
Result: Decreased p-STAT3 to nearly half of the control group at the concentration of 5 μM.
Reduced p-STAT3 levels in MDA-MB-231 cells in a dose-dependent manner.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 and 5 μM
Incubation Time: 0, 24 and 48 h
Result: Inhibited the migration of MDA-MB-231 cells, reducing wound closure to 9.65% after 24 h, compared to 24.51% in the control group.
Exhibited stronger inhibition than Belumosudil at 5 μM after 24 h, with cell migration rates of 3.48 % compared to 4.74 %.
Maintained a more prominent anti-metastatic effect than Belumosudil at 5 μM after 48 h, with cell migration rates of 9.33 % compared to 12.43 %.
分子量

582.70

Formula

C32H38N8O3
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-10 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:

ROCK2-IN-10ROCKSTATRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK2cytoskeletal organizationMDA-MB-231 cellsmetastasisSTAT3breast cancerInhibitorinhibitorinhibit

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