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  3. THK01

THK01 是一种有效的 ROCK2 抑制剂,对 ROCK2ROCK1IC50 值分别为 5.7 和 923 nM。THK01 通过 ROCK2-STAT3 信号通路抑制乳腺癌转移。THK01 可用于乳腺癌研究。

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THK01 Chemical Structure

THK01 Chemical Structure

CAS No. : 2226941-26-8

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  • 生物活性

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生物活性

THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1].

IC50 & Target[1]

ROCK2

5.7 nM (IC50)

ROCK1

923 nM (IC50)

体外研究
(In Vitro)

THK01 (1.25-10 μM; 48 h) 以剂量依赖的方式抑制 MDA-MB-231 细胞的迁移和侵袭能力[1]
THK01 (5 μM; 24 h; MDA-MB-231 细胞) 通过 STAT 信号通路抑制乳腺癌转移[1]
THK01 (1.25-10 μM; 24 h; MDA-MB-231 细胞) 以剂量依赖性方式下调 STAT3Y705 的磷酸化水平,同时略微上调 STAT3S727 的水平[1]

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Down-regulated the phosphorylation levels (p-STAT) of STAT1, STAT2, and STAT3, up-regulated of p-STAT5A and STAT6.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Reduced the level of p-STAT3Y705 and increased the expression of p-STAT3S727 in MDA-MB-231 cells.
体内研究
(In Vivo)

THK01 (15 mg/kg; i.v.; 雌性 BALB/c 裸鼠) 在体内抑制乳腺癌细胞转移[1]

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

Animal Model: Female BALB/c nude mice with MDAMB-231-Luc-mcherry xenografts (6 weeks old, weight about 20 g)[1]
Dosage: 15 mg/kg
Administration: Intravenous injection; once a day for 43 days
Result: Reduced the pulmonary metastasis of MDA-MB-231 in vivo with negligible toxicity.
分子量

327.34

Formula

C20H13N3O2

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
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  • 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.

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产品名称:
THK01
目录号:
HY-149266
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