RKI-1447
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
RKI-1447是一种强效ROCK 1和ROCK 2(Rho相关蛋白激酶1和2)抑制剂.
ROCK是一种丝氨酸-苏氨酸激酶;,通过作用于细胞骨架来调节细胞形态和运动.
RKI-1447特异性和剂量依赖性抑制ROCK1和ROCK2.RKI-1447抑制人癌细胞中ROCK底物MLC-2和MYPT-1的磷酸化.然而,在高达10 μmol/L的浓度下,它不影响AKT\MEK及S6激酶的磷酸化作用,表明其具有高特异性.此外,观察发现,RKI-1447选择性抑制LPA刺激后ROCK介导的细胞骨架重组,但不影响PDGF和缓激肽刺激后PAK介导的板状伪足和丝状伪足的形成.RKI-1447抑制乳腺癌细胞的迁移\侵袭和锚定非依赖性肿瘤生长[1].
在小鼠模型中,当肿瘤体积达到75至2300 mm3时,在肿瘤发病和开始治疗(连续14天,每天一次)时监测肿瘤,赋形剂(20% HPCD)或RKI-1447 (剂量为200 mg/kg/day)给药.赋形剂用药的小鼠肿瘤体积平均增加68.3%,但是,RKI-1447用药的小鼠肿瘤体积平均仅增加8.8%.因此,RKI-1447抑制了87%的乳腺肿瘤生长[1].
参考文献：
[1] Patel R A et al. , RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer. Cancer Res, 2012, 72(19): 5025-5034.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 326.37 |
| Cas No. | 1342278-01-6 |
| Formula | C16H14N4O2S |
| Synonyms | RKI 1447;RKI1447 |
| Solubility | insoluble in H2O; ≥16.3 mg/mL in DMSO; ≥6.32 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | RKI-1447是一种强效ROCK1/ROCK2抑制剂,IC50值分别为14.5 nM和6.2 nM. | |||||
| 靶点 | ROCK1 | ROCK2 | ||||
| IC50 | 14.5 nM | 6.2 nM | ||||
质量控制和MSDS
- 批次:
化学结构
