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PKC&ROCK

RKI-1447 (1342278-01-6)

RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.

Not Intended for Therapeutic Use. For research use only.

CAS: 1342278-01-6 Category

RKI-1447 (1342278-01-6) Description:

RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.

RKI-1447 binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppresses phosphorylation of the ROCK substrates mLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK and S6 kinase at concentrations as high as 10 μM. RKI-1447 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells.

RKI-1447 (1342278-01-6) Specifications:

Product Name RKI-1447
Synonym RKI-1447; RKI1447; RKI 1447. ROCK Inhibitor XIII.
Chemical Name 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 1342278-01-6
Molecular Formula C16H14N4O2S
Molecular Weight 326.37
Monoisotopic Mass 326.08375  g/mol
MDL number N/A
InChIKey GDVRVPIXWXOKQO-UHFFFAOYSA-N
InChi Code 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)
SMILES O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3
Form Solid powder
Color Yellow
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A potent inhibitor of the Rho-associated ROCK kinases

 

 

 

RIDADR NONH for all modes of transport

References:

[1]. Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 2012 Oct 1;72(19):5025-34. doi: 10.1158/0008-5472.CAN-12-0954. Epub 2012 Jul 30. PubMed PMID: 22846914; PubMed Central PMCID: PMC3463757.

[2]. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM. Cancer Res. 2012 Oct 1;72(19):5025-34. doi: 10.1158/0008-5472.CAN-12-0954. Epub 2012 Jul 30. PMID: 2284691

[3. RKI-1447, a Rho kinase inhibitor, causes ocular hypotension, actin stress fiber disruption, and increased phagocytosis. Dang Y, Wang C, Shah P, Waxman S, Loewen RT, Loewen NA. Graefes Arch Clin Exp Ophthalmol. 2019 Jan;257(1):101-109. doi: 10.1007/s00417-018-4175-6. Epub 2018 Nov 19. PMID: 30456419

[4]. Patel RA, 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 Oct 1;72(19):5025-34.

1 review for RKI-1447 (1342278-01-6)

  1. Cofttek

    Never had such good experience before,The RKI-1447 (1342278-01-6) is high purity,also customer service is pretty nice !gotta try!!

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