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RKI1447

Basic information Safety Supplier Related

RKI1447 Basic information

Product Name:
RKI1447
Synonyms:
  • CS-855
  • RKI 1447; RKI1447
  • RKI 1447
  • RKI1447
  • RKI-1447
  • 1-(3-HYDROXYBENZYL)-3-(4-(PYRIDIN-4-YL)THIAZOL-2-YL)UREA
  • Urea, N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-
  • 1-(3-Hydroxybenzyl)-3-[4-(pyridin-4-yl)thiazol-2-yl]urea RKI 1447
CAS:
1342278-01-6
MF:
C16H14N4O2S
MW:
326.37
EINECS:
200-256-5
Product Categories:
  • Inhibitors
Mol File:
1342278-01-6.mol
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RKI1447 Chemical Properties

Melting point:
>205oC (dec.)
Density 
1.408±0.06 g/cm3(Predicted)
storage temp. 
-20°C Freezer
solubility 
DMSO (Slightly), Methanol (Slightly, Heated)
pka
6.36±0.70(Predicted)
form 
Solid
color 
Pale Yellow to Pale Beige
InChI
InChI=1S/C16H14N4O2S/c21-13-3-1-2-11(8-13)9-18-15(22)20-16-19-14(10-23-16)12-4-6-17-7-5-12/h1-8,10,21H,9H2,(H2,18,19,20,22)
InChIKey
GDVRVPIXWXOKQO-UHFFFAOYSA-N
SMILES
N(CC1=CC=CC(O)=C1)C(NC1=NC(C2C=CN=CC=2)=CS1)=O
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RKI1447 Usage And Synthesis

Description

RKI-1447 is an inhibitor of the Rho-associated kinases ROCK1 and 2 (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase. In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase. Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).

Uses

RKI-1447 is a potent and selective ROCK1 and ROCK2 inhibitor with significant anti-invasive and anti-tumor activies.

References

[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.

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