1342278-01-6

Basic information

• Product Name: RKI1447
• Synonyms: RKI 1447;RKI1447;RKI-1447;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;RKI 1447 1-(3-Hydroxybenzyl)-3-[4-(pyridin-4-yl)thiazol-2-yl]urea;RKI-1447, >=98%;RKI-1447, 98%, a potent small molecule inhibitor of ROCK1 and ROCK2
• CAS NO: 1342278-01-6
• Molecular Formula: C₁₆H₁₄N₄O₂S
• Molecular Weight: 326.38
• EINECS: -0
• Product Categories: Inhibitors
• Mol File: 1342278-01-6.mol

Chemical Properties

• Appearance: /
• 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)
• CAS DataBase Reference: RKI1447(CAS DataBase Reference)
• NIST Chemistry Reference: RKI1447(1342278-01-6)
• EPA Substance Registry System: RKI1447(1342278-01-6)

Safety Data

• Hazardous Substances Data: 1342278-01-6(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
RKI-1447 is used as an anti-cancer agent for its potent and selective inhibition of ROCK1 and ROCK2. RKI1447 has shown significant anti-invasive and anti-tumor activities, making it a valuable asset in the development of cancer treatments. By suppressing the activation of ROCK substrates in cancer cells, RKI-1447 can help prevent tumor growth and progression.
Additionally, RKI-1447 can be used as a research tool for studying the role of ROCK1 and ROCK2 in various cellular processes, as well as for identifying potential therapeutic targets for other diseases associated with the dysregulation of these kinases.

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.

Upstream product

• 30235-28-0 4-pyridin-4-yl-thiazol-2-ylamine 
• 1342276-76-9 1-(3-methoxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea 
• 73604-31-6 3-hydroxybenzylamine 
• 1342277-18-2 phenyl 4-(pyridin-4-yl)thiazol-2-ylcarbamate 
• 5349-17-7 4-bromoacetylpyridine hydrobromide 

Downstream Products

• 1342278-90-3 1-(3-hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea methanesulfonate 
• 1342278-94-7 1-(3-hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea hydrochloride 

Relevant articles and documents

Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2)

Potent ROCK inhibitors of a new class of 1-benzyl-3-(4-pyridylthiazol-2-yl) ureas have been identified. Remarkable differences in activity were observed for ureas bearing a benzylic stereogenic center. Derivatives with hydroxy, methoxy and amino groups at the meta position of the phenyl ring give rise to the most potent inhibitors (low nM). Substitutions at the para position result in substantial loss of potency. Changes at the benzylic position are tolerated resulting in significant potency in the case of methyl and methylenehydroxy groups. X-Ray crystallography was used to establish the binding mode of this class of inhibitors and provides an explanation for the observed differences of the enantiomer series. Potent inhibition of ROCK in human lung cancer cells was shown by suppression of the levels of phosphorylation of the ROCK substrate MYPT-1.

PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE

Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.