產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	1342278-01-6
別名	RKI 1447;RKI1447
化學(xué)名	1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
分子式	C16H14N4O2S
分子量	326.37
溶解度	≥ 16.3 mg/mL in DMSO, ≥ 6.32 mg/mL in EtOH with ultrasonic and warming
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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