2. Stem Cell/Wnt TGF-beta/Smad
  3. RUNX
  4. Ro5-3335

Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.

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

CAS No. : 30195-30-3

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Ro5-3335:

Ro5-3335 Related Antibodies

Top Publications Citing Use of Products

    Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 16;15(1):8114.

    Western blotting for scWAT RUNX1 protein in WT (dark gray) and Tg6 (red) mice treated with RUNX1 inhibitor Ro5-3335 (5 mg/kg; s.c.; every other day for six times) or DMSO control. Ro5-3335 attenuated the increase in RUNX1 protein in scWAT of Tg6-mice compared with WT-mice.

    Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 16;15(1):8114.

    Lipid metabolism gene expression (qPCR) in scWAT of WT and Tg6-mice treated with RUNX1 inhibitor Ro5-3335 (5 mg/kg; s.c.; every other day for six times). Ro5-3335 administration attenuated the changes observed in Tg6-mice associated with high EPO on expression of lipid metabolismgenes.

    Ro5-3335 purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4256-4277.  [Abstract]

    ApoE-/- mice receiving HFD for 8 weeks were treated with Ro5-3335 (25 mg/kg; i.p.; twice a week for 4 weeks; DMSO) or DMSO starting at week 8. Representative images and quantification of atherosclerotic area in cross-sections of aortic root of ApoE-/- mice treated with Ro5-3335 and DMSO by HE, Oil Red O and Masson staining.

    Ro5-3335 purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4256-4277.  [Abstract]

    Representative images of immunofluorescence co-staining for RUNX1 together with macrophage maker F4/80 and M2 macrophage marker CD206 in aortic root plaques from ApoE-/- mice treated with Ro5-3335 (25 mg/kg; i.p.; twice a week for 4 weeks; DMSO) and DMSO, with quantification of immunofluorescence intensity.

    Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Dec;24(12):2042-2052.  [Abstract]

    MEPs were isolated from healthy C57BL/6J mice and treated with Kyn or Kyn combined with the RUNX1 inhibitor Ro5-3335 (2 μM) in collagen medium for 7 d, and a c.f.u. analysis was performed.

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    Description

    Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation[1].

    IC50 & Target

    RUNX1

     

    Cellular Effect
    Cell Line Type Value Description References
    H9 IC50
    0.6 μM
    Compound: 1
    Inhibition of HIV replication in H9 cells.
    Inhibition of HIV replication in H9 cells.
    		[PMID: 7650672]
    H9 IC50
    0.6 μM
    Compound: 1
    Inhibition of HIV-1 replication in H9 cells infected with three different concentrations of HIV IIIB strain
    Inhibition of HIV-1 replication in H9 cells infected with three different concentrations of HIV IIIB strain
    		[PMID: 8410982]
    SW480 IC50
    4 μM
    Compound: 1
    The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay
    The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay
    		[PMID: 7650672]
    In Vitro

    Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively[1].
    Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos[1].
    Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex[1].

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

    Ro5-3335 Related Antibodies
    In Vivo

    Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models[1].
    Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish[1].
    Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model[1].

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

    Animal Model: C57BL/6 mice (leukemic model)[1]
    Dosage: 300 mg/kg
    Administration: Oral administration; daily; for 30 days
    Result: Reduced the number of c-kit+ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen.
    Molecular Weight

    259.69

    Formula

    C13H10ClN3O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CN3)=NC1
    Shipping

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

    DMSO : 100 mg/mL (385.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.8507 mL 19.2537 mL 38.5075 mL
    5 mM 0.7701 mL 3.8507 mL 7.7015 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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 (9.63 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 (9.63 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

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    (per animal)

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
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    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.
    Purity & Documentation

    Purity: 99.52%

    SDS (393 KB)

    COA (258 KB) HNMR (273 KB) RP-HPLC (256 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    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 3.8507 mL 19.2537 mL 38.5075 mL 96.2686 mL
    5 mM 0.7701 mL 3.8507 mL 7.7015 mL 19.2537 mL
    10 mM 0.3851 mL 1.9254 mL 3.8507 mL 9.6269 mL
    15 mM 0.2567 mL 1.2836 mL 2.5672 mL 6.4179 mL
    20 mM 0.1925 mL 0.9627 mL 1.9254 mL 4.8134 mL
    25 mM 0.1540 mL 0.7701 mL 1.5403 mL 3.8507 mL
    30 mM 0.1284 mL 0.6418 mL 1.2836 mL 3.2090 mL
    40 mM 0.0963 mL 0.4813 mL 0.9627 mL 2.4067 mL
    50 mM 0.0770 mL 0.3851 mL 0.7701 mL 1.9254 mL
    60 mM 0.0642 mL 0.3209 mL 0.6418 mL 1.6045 mL
    80 mM 0.0481 mL 0.2407 mL 0.4813 mL 1.2034 mL
    100 mM 0.0385 mL 0.1925 mL 0.3851 mL 0.9627 mL
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    Ro5-3335 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:

    Ro5-333530195-30-3RUNXRunt-related transcription factorscorebindingfactorCBFleukemiaRUNX1CBFβRUNX1-CBFBinteractionInhibitorinhibitorinhibit

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