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

CAS No. : 1782109-09-4

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Top Publications Citing Use of Products

Publications Citing Use of MCE RKI-1447 dihydrochloride

    RKI-1447 dihydrochloride purchased from MCE. Usage Cited in: Med Sci Monit. 2020 Feb 6;26:e919220.

    The effects of RKI-1447 on glucose tolerance and insulin resistance in a mouse model of nonalcoholic fatty liver disease (NAFLD) induced by a high-fat diet. The expression of the insulin receptor substrate-1 (IRS1) are shown. The mice were fed with a high-fat diet for 12 weeks. From the ninth week, the mice were treated orally with the ROCK inhibitor RKI-1447 (2 mg/kg to 8 mg/kg) twice weekly for three weeks.

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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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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

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