2. Cell Cycle/DNA Damage Stem Cell/Wnt Cytoskeleton TGF-beta/Smad
  3. ROCK
  4. ROCK2-IN-14

ROCK2-IN-14 是一种口服有效、选择性 ROCK2 抑制剂 (IC50=4.8 nM)，对 ROCK1 的选择性是 212 倍 (IC50=1.01 μM)。ROCK2-IN-14 通过抑制 ROCK2/S100A9 信号通路，下调 S100A9 表达，抑制 NM2 磷酸化并恢复细胞骨架异常。进而，ROCK2-IN-14 可降低炎症因子水平、减轻皮肤炎症，发挥抗炎活性。ROCK2-IN-14 还显著抑制特应性皮炎 (AD) 模型小鼠的耳厚增厚、降低 IgE、TNF-α、IL-6 及 TSLP 水平。ROCK2-IN-14 的安全性良好，其最大耐受口服剂量超过 500 mg/kg。ROCK2-IN-14 可用于特应性皮炎的研究。

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ROCK2-IN-14

ROCK2-IN-14 Chemical Structure

CAS No. : 3115784-59-0

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ROCK2-IN-14 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 has a good safety profile, with a maximum tolerated oral dose exceeding 500 mg/kg. ROCK2-IN-14 can be used for research on atopic dermatitis[1].

IC50 & Target[1]

ROCK2

4.8 nM (IC50)

体外研究
(In Vitro)

ROCK2-IN-14 (compound 10d) (10 nM-1 μM; 24 h) 可显著抑制 HaCaT 细胞中 S100A9、p-MYPT1 和 p-NM2 的蛋白表达水平[1]。
ROCK2-IN-14 (10 nM-1 μM; 48 h) 可呈浓度依赖性降低 HaCaT 细胞中 IL-6 和 TSLP 的 mRNA 表达水平[1]。

ROCK2-IN-14 (10 nM-1 μM; 24 h) 可显著改善 HaCaT 细胞中细胞骨架 F-肌动蛋白的异常聚合，该结果由 IF 实验观察得出[1]。
ROCK2-IN-14 (1 nM-1 μM; 72 h) 对 HaCaT 细胞的活力无显著影响，所有组别的细胞存活率均高于 90%[1]。
ROCK2-IN-14 (1 μM; 24 h) 可显著降低 HaCaT 细胞的迁移能力，与对照组相比，划痕愈合率下降约 45%[1]。

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

ROCK2-IN-14 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: HaCaT
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 72 h
Result: Did not significantly affect the viability of HaCaT cells, and the cell survival rate was higher than 90% at all tested concentrations.

Real Time qPCR[1]

Cell Line: HaCaT
Concentration: 10 nM, 100 nM, 1 μM
Incubation Time: 48 h
Result: Reduced the mRNA expression levels of inflammatory factors IL-6 and TSLP in a concentration-dependent manner, with the most significant reduction at 1 μM (by 68% and 72%, respectively).

Western Blot Analysis[1]

Cell Line: HaCaT
Concentration: 48 h
Incubation Time: 24 h
Result: Significantly downregulated the protein expression levels of S100A9, p-MYPT1 (Thr853), and p-NM2 in HaCaT cells in a concentration-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-∞ Tmax Cmax F
Mice[1] 2 mg/kg i.v. 1.39 h 448.34 ng·h/mL / / /
Mice[1] 25 mg/kg p.o. 2.94 h 534.68 ng·h/mL 0.63 h 182.5 ng/mL 9.54 %
体内研究
(In Vivo)

ROCK2-IN-14 (compound 10d) (10 mg/kg, 30 mg/kg, 100 mg/kg; 口服; 每日 1 次, 14 天) 可显著降低特应性皮炎 (AD) 模型 BALB/c 小鼠的耳肿胀程度，并下调其血清中 IgE、TNF-α、IL-6 及 TSLP 的水平[1]。
ROCK2-IN-14 (500 mg/kg; 口服; 单剂量) 在 ICR 小鼠急性毒性模型中未表现出明显毒性反应，小鼠存活率为 100%，最大耐受剂量超过 500 mg/kg[1]。

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

Animal Model: BALB/c mice (female, 18-22 g, 6-8 weeks old) + Atopic Dermatitis (AD) model[1]
Dosage: 10 mg/kg (0.5% CMC-Na), 30 mg/kg (0.5% CMC-Na), 100 mg/kg (0.5% CMC-Na)
Administration: 14 consecutive days of oral gavage administration once daily
Result: Significantly reduced the ear thickness increase of AD model mice by 35% (10 mg/kg), 58% (30 mg/kg) and 72% (100 mg/kg), compared with the model group; serum levels of IgE, TNF-α, IL-6 and TSLP were decreased by 28%, 42%, 51% and 48% at 30 mg/kg dosage, respectively.
Animal Model: ICR mice (male and female, 20-24 g, 7-9 weeks old) + Acute toxicity model[1]
Dosage: 500 mg/kg
Administration: single oral gavage administration
Result: No obvious toxic symptoms (such as weight loss, abnormal behavior, organ damage) were observed in mice within 14 days of observation, and the survival rate of mice was 100%, indicating that the maximum tolerated dose (MTD) was more than 500 mg/kg.
分子量

434.55

Formula

C24H26N4O2S
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

ROCK2-IN-14 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-143115784-59-0ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK1ROCK2atopic dermatitisS100A9Inhibitorinhibitorinhibit

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