Cell Cycle/Checkpoint ROCK RKI-1447


Catalog No. T1898   CAS 1342278-01-6
Synonyms: RKI1447, RKI 1447,
Purity 99.73% Datasheet

RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.

RKI-1447, CAS 1342278-01-6
Pack Size Availability Price/USD Quantity
2 mg In stock 51.00
5 mg In stock 91.00
10 mg In stock 122.00
25 mg In stock 220.00
50 mg In stock 428.00
100 mg In stock 727.00
1 mL * 10 mM (in DMSO) In stock 91.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
Targets&IC50 ROCK1 :ic50 14.5nM,   ROCK2 :ic50 6.2nM,  
Kinase Assay Z-Lyte FRET kinase assay: Kinase inhibition is measured using the Invitrogen Z-Lyte® FRET kinase assay with Ser/Thr 13 peptide substrate based on the myosin light chain sequence KKRPQRRYSNVF. Compounds are tested on three separate days with 8 point dilutions performed in duplicate to determine average IC50 values. The assay conditions are optimized to 15 μL of kinase reaction volume with 5 ng of enzyme in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reaction is incubated for 1 h at room temperature in the presence of 1.5 μM of peptide substrate with 12.5 μM of ATP (for ROCK1) or 2 μM of substrate with 50 μM of ATP (for ROCK2). The reaction is then stopped and the ratio of phosphorylated to unphosphorylated peptides is determined by selective cleavage of only the unphosphorylated peptide as described by the manufacturer. This is followed by excitation of coumarin at 400 nm resulting in emission at 445 nm and energy transfer to fluorescein and final emission at 520 nm. The substrate contains both coumarin and fluorescein and only uncleaved phosphorylated substrate will undergo FRET. The ratio of the signals at 445 nm and 520 nm is measured using a Wallac EnVision Plate Reader, model 2102 plate-reader.
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 (2mg/ml) is added to each well and incubated for 3 hours. After incubation the plates are read at 540 nm. (Only for Reference)
Cell lines: MDA-MB-231
Animal Research
Animal Model: MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J]
Synonyms RKI1447, RKI 1447,
Purity 98.00%
Appearance solid
Molecular Weight 326.37
Formula C16H14N4O2S
CAS No. 1342278-01-6


-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 60 mg/mL (183.8 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

15% Captisol: 30 mg/mL


References and Literature
1. Patel RA, et al. Cancer Res, 2012, 72(19), 5025-5034. 2. Pireddu R, et al. Medchemcomm, 2012, 3(6), 699-709.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library

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