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RKI-1447

  Cat. No.:  DC7269   Featured
Chemical Structure
1342278-01-6
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More than 5000 active chemicals with high quality for research!
Field of application
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1342278-01-6
Chemical Name: Urea,N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-
Synonyms: RKI 1447; RKI1447
SMILES: C1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3
Formula: C16H14N4O2S
M.Wt: 326.37
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
In Vivo: RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. RKI-1447 inhibits mammary tumor growth by 87% and on average the mammary tumors from RKI-1447 treated mice are 7.7 fold smaller compared to those tumors from mice treated with the vehicle control[1].
In Vitro: 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 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[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1028 Y-27632 2HCL Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM.
DC6902 Thiazovivin Thiazovivin is a rock inhibitor and enhances fibroblast reprogramming efficiency to generate stem cells
DC7246 SR3677 SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.
DC8329 SLx-2119(KD-025,Belumosudil ) SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM)
DC9854 SAR407899 SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
DC7269 RKI-1447 RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
DC8831 RKI-1313 RKI-1313 is the negative control for RKI-1447 which is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer
DC7774 Ripasudil(K-115) K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.
DC9614 Hydroxyfasudil (hydrochloride) Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
DC7144 GSK429286A GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
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