A ROCK1 and ROCK2 inhibitor
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RKI-1447

Item No. 16278

Technical Information
Formal Name
N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-urea
CAS Number
1342278-01-6
Molecular Formula
C16H14N4O2S
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
228, 265 nm
SMILES
OC1=CC(CNC(NC2=NC(C3=CC=NC=C3)=CS2)=O)=CC=C1
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)
InChi Key
GDVRVPIXWXOKQO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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.1 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.1 Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Patel, R.A., Forinash, K.D., Pireddu, R., et alRKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and anti-tumor activities in breast cancer. Cancer Res. 72(19), 5025-5034 (2012).