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RKI-1447

现货
Catalog No.
A3771
ROCK1/ROCK2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 990.00
现货
5mg
¥ 600.00
现货
10mg
¥ 1,100.00
现货
25mg
¥ 2,400.00
现货
50mg
¥ 4,000.00
Ship with 10-15 days

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Background

RKI-1447 is a potent inhibitor of ROCK 1 and 2 (Rho-associated protein kinase 1 and 2).

ROCK is a serine-threonine kinase, which regulates cell shape and movement via acting on cytoskeleton.

RKI-1447 specifically and dose-dependently inhibits ROCK1 and ROCK2. RKI-1447 inhibited the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells. However, it does not affect the phosphorylation of the AKT, MEK, and S6 kinase at a high concentrations of 10 μmol/L. It indicated a high specificity. Additionally, it was also observed that RKI-1447 selectively suppressed ROCK-mediated cytoskeleton re-organization following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation. RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells [1]

In mouse model, tumors were monitored at the time of tumor onset and the beginning of treatment (once a day for 14 days) with vehicle (20% HPCD) or RKI-1447 (200 mg/kg/day), when tumor volumes reached 75 to 2,300 mm3. Tumors from mice treated with vehicle increased in average tumor volume of 68.3% but tumors from mice treated with the RKI-1447 increased in average tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87% [1].

Reference:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt326.37
Cas No.1342278-01-6
FormulaC16H14N4O2S
SynonymsRKI 1447;RKI1447
Solubility≥16.3 mg/mL in DMSO, ≥6.32 mg/mL in EtOH with ultrasonic and warming, <1.8 mg/mL in H2O
Chemical Name1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
SDFDownload SDF
Canonical SMILESC1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

生物活性

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        

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