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

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1342278-01-6

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무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 4 publication(s) in Google Scholar

Other Forms of RKI-1447:

RKI-1447 Related Antibodies

Top Publications Citing Use of Products

    RKI-1447 purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2020 Feb 6;26:e919220.  [Abstract]

    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.

    View All ROCK Isoform Specific Products:

    View All Isoforms
    ROCK ROCK1 ROCK2

    • Biological Activity

    • Protocol

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.

    IC50 & Target[1]

    ROCK2

    6.2 nM (IC50)

    ROCK1

    14.5 nM (IC50)

    In Vitro

    RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. 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. RKI-1447 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells[1].

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

    RKI-1447 Related Antibodies
    In Vivo

    RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. RKI-1447 inhibits mammary tumor growth by 87% and on average the mammary tumors from RKI-1447 treated mice are 7.7 fold smaller compared to those tumors from mice treated with the vehicle control[1].

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

    326.37

    화학식

    C16H14N4O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    용액&용해도
    In Vitro: 

    DMSO : ≥ 50 mg/mL (153.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0640 mL 15.3200 mL 30.6401 mL
    5 mM 0.6128 mL 3.0640 mL 6.1280 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 몰농도 계산기

    • 농도 희석 계산기

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서
    References
    Kinase Assay
    [1]

    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. The ratio of the signals at 445 nm and 520 nm is measured. IC50 values are determined using fitted curves with GraphPad Prism 5 software[1].

    MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    Cell Assay 
    [1]

    NIH 3T3 cells are plated at 8000 cells/well in 8-chamber slides in serum free media for 24 hours, and treated with vehicle, 1 μM RKI-1447 or 1 μM RKI-1313 for 1 hour. The cells are then stimulated with complete media, 10 μM LPA, 200 ng/mL bradykinin or 30 ng/mL PDGF for 30 mins. After stimulation, the cells are fixed in 4% paraformaldehyde and stained with Texas-Red Phalloidin. Mounting medium containing DAPI is then added and at least 100 cells per well are observed[1].

    MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    Animal Administration
    [1]

    Mice: MMTV/neu transgenic mice are treated i.p. daily for 14 days with either Vehicle [20%-2-hydroxypropyl-beta-cyclodextrin (HPCD)] or 200 mpk RKI-1447 dissolved in freshly prepared HPCD. The percent change in volume is calculated on the basis of the tumor volume on the last day of treatment (Vf) relative to that on the day of initiation of treatment (V0). The average percent change in tumor volume is then calculated for each treatment group[1].

    MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0640 mL 15.3200 mL 30.6401 mL 76.6002 mL
    5 mM 0.6128 mL 3.0640 mL 6.1280 mL 15.3200 mL
    10 mM 0.3064 mL 1.5320 mL 3.0640 mL 7.6600 mL
    15 mM 0.2043 mL 1.0213 mL 2.0427 mL 5.1067 mL
    20 mM 0.1532 mL 0.7660 mL 1.5320 mL 3.8300 mL
    25 mM 0.1226 mL 0.6128 mL 1.2256 mL 3.0640 mL
    30 mM 0.1021 mL 0.5107 mL 1.0213 mL 2.5533 mL
    40 mM 0.0766 mL 0.3830 mL 0.7660 mL 1.9150 mL
    50 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.5320 mL
    60 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
    80 mM 0.0383 mL 0.1915 mL 0.3830 mL 0.9575 mL
    100 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.7660 mL
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    RKI-1447 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    RKI-14471342278-01-6RKI1447RKI 1447ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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    상품명:
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    Cat. No.:
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