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RKI-1447

Catalog No. T1898 CAS 1342278-01-6

Synonyms: RKI1447

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

RKI-1447, CAS 1342278-01-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 435.00
200 mg	In stock	$ 548.00
500 mg	In stock	$ 885.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.73%

Purity: 99.56%

Purity: 99.18%

Purity: 98.99%

Purity: 98.75%

Purity: 98.59%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
Targets&IC50	ROCK1:14.5 nM, ROCK2:6.2 nM
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%.
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.
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 (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)

Synonyms	RKI1447
Molecular Weight	326.37
Formula	C16H14N4O2S
CAS No.	1342278-01-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (183.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

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：

TGF-beta/Smad Compound Library Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Anti-Cancer Compound Library Kinase Inhibitor Library Anti-Aging Compound Library

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Related compounds with same targets

RKI1313 WAY-656935 SB-772077B dihydrochloride ROCK-IN-2 Tofacitinib ROCK2-IN-6 URMC-099 Cotosudil

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RKI-1447 1342278-01-6 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK Rho-kinase Inhibitor inhibit ROK Rho-associated kinase RKI1447 Rho-associated protein kinase RKI 1447 inhibitor

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