RKI-1447|cas 1342278-01-6| DC Chem|Supplier|Price|Buy

RKI-1447|cas 1342278-01-6| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: RKI-1447|cas 1342278-01-6,Purity: >98% ,Cat No. DC7269, In stock.

Contact: website:www.dcchemicals.com,

sales@dcchemicals.com,order@dcchemicals.com,info@dcchemicals.com,

Tel: +86-21-61454686;Fax:+86-21-61642738；

RKI-1447|cas 1342278-01-6 ,Synonym: RKI 1447; RKI1447  ,Chemical name: Urea,N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]- ,Molecular Formula: C16H14N4O2S ,MW:326.37

RKI-1447, cas 1342278-01-6,Purity: >98%, Best Price and quality from DC Chemicals. RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.

RKI-1447 is a cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting Rho Kinase inhibitor, displaying much reduced potency against PKA, PKN1/PRK1, p70S6K/RPS6kB1, AKT1, MRCKa/CDC42BPA (85.5%, 80.5%, 61.9%, 56.0%, and 50.4% inhibition, respectively, by 1 ?M RKI-1447) or 15 other kinases. Crystal structures of the RKI-1447/ROCK1 complex reveals that 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 suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had 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 (actin stress fiber formation) following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells. [1] RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. Tumors from mice treated with the RKI-1447 increases in size with an average percent change in tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87%, and on average the mammary tumors from Compared with those tumors from mice treated with the vehicle control, RKI-1447 treated mice are 7.7-fold smaller. RKI-1447 treatments does not result in mouse weight loss. [1]