RKI-1447

SKU: orb1307195

Description

RKI-1447 is a selective small molecule inhibitor targeting ROCK1 and ROCK2 kinases. It demonstrates anti-invasive and anti-tumor properties, making it a valuable research tool for studying cancer cell migration, metastasis, and tumor progression in both cellular and animal models.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1342278-01-6
• MW: 326.37
• Purity: 99.56%
• Formula: C₁₆H₁₄N₄O₂S
• SMILES: Oc1cccc(CNC(=O)Nc2nc(cs2)-c2ccncc2)c1
• Target: ROCK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.13 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:18.33 mg/mL (56.16 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ROCK1:14.5 nM|ROCK2:6.2 nM
• In Vivo:
  RKI-1447 inhibits the phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, without affecting the phosphorylation levels of AKT, MEK, and S6 kinases at concentrations up to 10 μM. It suppresses the migration, invasion, and anchorage-independent growth of breast cancer cells. The crystal structure of the RKI-1447/ROCK1 complex reveals that RKI-1447 is a type I kinase inhibitor, binding to the ATP site through interactions with the hinge region and DFG motif.
• In Vitro:
  RKI-1447 inhibits the growth of 87% of breast tumors, reducing the average volume of breast tumors by 7.7 times compared to the control mice. In a transgenic mouse model, RKI-1447 effectively suppresses breast tumor growth. When tumors in mice are treated with RKI-1447, the average percentage increase in tumor volume is only 8.8%.
• Cell Research:
  Cells are plated in a 96 well tissue culture plate (1200 cells per well) and incubated for 24 hours. After incubation the cells are treated with vehicle or increasing concentrations of RKI-1447 for 72 hours. After incubation, freshly prepared MTT (2 mg/ml) is added to each well and incubated for 3 hours. After incubation the plates are read at 540 nm. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RKI 1447, RKI1447, RKI-1447, ROCK, ROCK1, ROCK2, ROK, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, inhibit, Inhibitor

Compound Identifiers

PubChem CID

60138149