RKI-1447

SKU: orb1307195

描述

RKI-1447 is a selective small molecule inhibitor targeting ROCK1 and ROCK2 kinases. It demonstrates anti-invasive and anti-tumor properties, making it a valuable research tool for studying cancer cell migration, metastasis, and tumor progression in both cellular and animal models.

研究领域

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	1342278-01-6
MW	326.37
纯度	99.73% (May vary between batches)
分子式	C₁₆H₁₄N₄O₂S
SMILES	Oc1cccc(CNC(=O)Nc2nc(cs2)-c2ccncc2)c1
靶点	ROCK
溶解性	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.13 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:18.33 mg/mL (56.16 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

生物活性

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靶点 IC50	ROCK1:14.5 nM\|ROCK2:6.2 nM
体内	RKI-1447 inhibits the phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, without affecting the phosphorylation levels of AKT, MEK, and S6 kinases at concentrations up to 10 μM. It suppresses the migration, invasion, and anchorage-independent growth of breast cancer cells. The crystal structure of the RKI-1447/ROCK1 complex reveals that RKI-1447 is a type I kinase inhibitor, binding to the ATP site through interactions with the hinge region and DFG motif.
体外	RKI-1447 inhibits the growth of 87% of breast tumors, reducing the average volume of breast tumors by 7.7 times compared to the control mice. In a transgenic mouse model, RKI-1447 effectively suppresses breast tumor growth. When tumors in mice are treated with RKI-1447, the average percentage increase in tumor volume is only 8.8%.
细胞研究	Cells are plated in a 96 well tissue culture plate (1200 cells per well) and incubated for 24 hours. After incubation the cells are treated with vehicle or increasing concentrations of RKI-1447 for 72 hours. After incubation, freshly prepared MTT (2 mg/ml) is added to each well and incubated for 3 hours. After incubation the plates are read at 540 nm. (Only for Reference)

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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RKI 1447, RKI1447, RKI-1447, ROCK, ROCK1, ROCK2, ROK, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, inhibit, Inhibitor

相似产品

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RKI-1447 dihydrochloride [orb1688133]
CAS 号：
1782109-09-4
MW:
399.29
分子式：
C₁₆H₁₆Cl₂N₄O₂S
可选规格： 2 mg
RKI-1447 [orb1226505]
纯度：
>98% (HPLC)
CAS 号：
1342278-01-6
MW:
326.37
分子式：
C₁₆H₁₄N₄O₂S
可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

60138149 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	1782109-09-4
MW:	399.29
分子式：	C₁₆H₁₆Cl₂N₄O₂S

纯度：	>98% (HPLC)
CAS 号：	1342278-01-6
MW:	326.37
分子式：	C₁₆H₁₄N₄O₂S

RKI-1447

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

RKI-1447 dihydrochloride [orb1688133]

RKI-1447 [orb1226505]

质量保证

化合物标识

关键属性

实验方案信息

可选规格