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RKI-1447

In stock
Catalog No.
A3771
Potent ROCK1/ROCK2 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$99.00
In stock
5mg
$60.00
In stock
10mg
$110.00
In stock
25mg
$240.00
In stock
50mg
$400.00
In stock

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Email: [email protected]

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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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description RKI-1447 is a potent inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
Targets ROCK1 ROCK2        
IC50 14.5 nM 6.2 nM        

Quality Control

Chemical structure

RKI-1447