1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Cytoskeleton
    TGF-beta/Smad
    Apoptosis
  2. ROCK
    Apoptosis
  3. RKI 1447 dihydrochloride

RKI 1447 dihydrochloride 

Cat. No.: HY-110339
Handling Instructions

RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.

For research use only. We do not sell to patients.

RKI 1447 dihydrochloride Chemical Structure

RKI 1447 dihydrochloride Chemical Structure

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Description

RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively[1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis[2].

IC50 & Target[1][2]

ROCK1

14.5 nM (IC50)

ROCK2

6.2 nM (IC50)

Apoptosis

 

In Vitro

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[1].
RKI 1447 (0.003-10 μM) is potent at inhibiting the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells[1].
RKI 1447 exhibits effective anticancer activity in colorectal carcinoma (CRC). RKI 1447 (10-320 μM; 24 hours) drastically suppresses HCT-8 and HCT-116 cell growth[2].
RKI 1447 (20-80 μM; 24 hours) induces apoptosis in a dose-dependent manner[2].

Cell Viability Assay[2]

Cell Line: CRC cell lines HCT-8 and HCT-116 cells
Concentration: 0, 10, 20, 40, 80, 160, 320 μM
Incubation Time: 24 hours
Result: HCT-8 and HCT-116 viability was drastically decreased in a dose-dependent manner.

Apoptosis Analysis[2]

Cell Line: CRC cell lines HCT-8 and HCT-116 cells
Concentration: 0, 20, 40, 80 μM
Incubation Time: 24 hours
Result: Treatment promoted apoptosis.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 human breast cancer cells
Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3 ,10 μM
Incubation Time:
Result: Decreased the levels of P-MLC-2, but not total MLC-2, in a concentration-dependent manner with significant effects starting at 100 nM.
In Vivo

RKI 1447 (200 mg/kg; i.p. daily for 14 days) inhibits mammary tumor growth in vivo[1].
RKI 1447 (100 mg/kg; i.p.; once every 3 days; for 14 days) exerts antitumor activity on CRC in vivo. RKI 1447 does not exert physiological toxicity on the mice[2].

Animal Model: MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J][1]
Dosage: 200 mg/kg
Administration: Treated i.p. daily for 14 days
Result: Tumors from mice treated with vehicle increased in size with an average percent change in tumor volume of 68.3%. In contrast, tumors from mice treated with the RKI-1447 increased in size with an average percent change in tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87%.
Animal Model: 5-week-old Male BALB/C nude mice[2]
Dosage: 100 mg/kg
Administration: Intraperitoneally injected; once every 3 days; for 14 days
Result: Efficiently blocked CRC tumor growth in vivo.
Molecular Weight

399.29

Formula

C₁₆H₁₆Cl₂N₄O₂S

SMILES

O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vivo:
  • 1.

    RKI-1447 dissolved in freshly prepared 20% 2-hydroxypropyl-beta-cyclodextrin (HPCD)[1].

References
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Keywords:

RKI 1447RKI1447RKI-1447ROCKApoptosisRho-associated protein kinaseRho-associated kinaseRho-kinaseROKmigrationinvasionbreastcancercolorectalcarcinomacellularbioenergeticsERstressmitochondrialdysfunctionInhibitorinhibitorinhibit

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Product Name:
RKI 1447 dihydrochloride
Cat. No.:
HY-110339
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