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  3. KRIBB11

KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.

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

KRIBB11 Chemical Structure

KRIBB11 Chemical Structure

CAS No. : 342639-96-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 96 In-stock
25 mg USD 216 In-stock
50 mg USD 360 In-stock
100 mg USD 648 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

Top Publications Citing Use of Products

    KRIBB11 purchased from MedChemExpress. Usage Cited in: Arch Biochem Biophys. 2023 Jan 23;109525.  [Abstract]

    KRIBB11 (0, 10, 20 µM; 24 h)completely blocks n-butyrate-mediated HSP70 expression and Hspa1α promoter activation in Caco-2 cells (fig B and C).

    KRIBB11 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Dec 12;8(12):3203.  [Abstract]

    Immunoblot showing that HSF1 inhibitor KRIBB11 and transcription inhibitor Act-D both fail to block RIP140 degradation.

    KRIBB11 purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Oct;11(10):1475-1492.  [Abstract]

    (A) IHC staining of N-cadherin and E-cadherin in the pancreas from KPC mice treated with vehicle, Metformin, or KRIBB11. (B) Masson's trichrome staining and IHC staining of α-SMA in pancreatic tissues from mice treated with vehicle, Metformin, or KRIBB11.

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.

    IC50 & Target[1]

    HSF1

    1.2 μM (IC50)

    In Vitro

    KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70. KRIBB11 induces growth arrest and apoptosis of HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of p-TEFb (positive transcription elongation factor b) to the hsp70 promoter[1]. PARP and caspase-3 cleavage is increased in cells treated with KRIBB11. Incubating RKO with KRIBB11, shows a toxic threshold of about 10 μM, and an IC50 of 20-30 μM[2].

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

    In Vivo

    KRIBB11 (50 mg/kg, i.p.) results in a 47.4% inhibition of tumor growth in nude mice, without body weight loss[1].

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

    Molecular Weight

    284.27

    Formula

    C13H12N6O2

    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    CNC1=CC=C([N+]([O-])=O)C(NC2=CC3=C(NN=C3)C=C2)=N1

    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 : 125 mg/mL (439.72 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 3.5178 mL 17.5889 mL 35.1778 mL
    5 mM 0.7036 mL 3.5178 mL 7.0356 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 (8.79 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.
    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.
    Purity & Documentation

    Purity: 99.54%

    References
    Kinase Assay
    [1]

    HCT-116 cells are washed with PBS and then homogenized with a 27-gauge syringe in binding buffer (10 mm Tris-HCl (pH 7.4), 50 mm KCl, 5 mm MgCl2, 1 mm EDTA, and 0.1 mm Na3VO4). The cell lysate is centrifuged at 13,000 rpm for 30 min at 4°C, and the supernatant is collected. The HCT-116 cell lysate supernatant is precleared by incubating with Dynabeads M-280 streptavidin for 30 min at 4°C and captured by magnet separation. The cleared supernatants are incubated with biotinyl-KRIBB11 compound. After overnight incubation at 4°C, proteins associated with the biotinyl-KRIBB11 compound are precipitated with Dynabeads M-280 streptavidin. Precipitated samples are separated by a magnet. Samples are washed with 1 mL of ishing buffer containing 50 mm HEPES (pH 7.5), 50 mm NaCl, 1 mm EDTA, 1 mm EGTA, 0.1% Tween 20, 10% (v/v) glycerol, 1 mm NaF, 0.1 mm Na3VO4, and protease inhibitor mixture tablets (1 tablet/10 mL). Samples are boiled in SDS-PAGE sample buffer, separated by 10% polyacrylamide gel, and immunoblotted with antibodies against HSF1, HSF2, HSP90, or CDK9.

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

    Cell Assay
    [1]

    Cells are seeded onto 96-well plates at a density of 6×103 cells per well in McCoy's 5A medium with 10% FBS. After 24 h, the medium is replenwashed with fresh complete medium containing chemicals or 0.1% DMSO. After incubation for 48 h, the cell proliferation reagent WST-1 is added to each well. The amount of WST-1 formazan produced is measured at 450 nm using an ELISA reader.

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

    Animal Administration
    [1]

    Seven-week-old female inbred specific pathogen-free Balb/c nude mice are housed under sterile conditions with 12-h light/dark cycles, and fed food and water ad libitum. For the evaluation of the in vivo anti-tumor activity of KRIBB11, HCT-116 cells (0.3 mL of 4×107 cells/mL) are implanted subcutaneously into the right flank of the mice on day 0. KRIBB11 is dissolved in 10% dimethylacetamide, 50% PEG300, and 40% distilled water. When the size of tumors reached 72.2 mm3, the compound is administered intraperitoneally at a dose of 50 mg/kg/day for 18 days. Tumor volumes are estimated by using the formula length (mm) × width (mm) × height (mm)/2. To determine the toxicity of the compound, the body weight of tumor-bearing animals is recorded. On day 18, the mice are sacrificed, and the tumors are weighed.

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

    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 3.5178 mL 17.5889 mL 35.1778 mL 87.9446 mL
    5 mM 0.7036 mL 3.5178 mL 7.0356 mL 17.5889 mL
    10 mM 0.3518 mL 1.7589 mL 3.5178 mL 8.7945 mL
    15 mM 0.2345 mL 1.1726 mL 2.3452 mL 5.8630 mL
    20 mM 0.1759 mL 0.8794 mL 1.7589 mL 4.3972 mL
    25 mM 0.1407 mL 0.7036 mL 1.4071 mL 3.5178 mL
    30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9315 mL
    40 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1986 mL
    50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7589 mL
    60 mM 0.0586 mL 0.2931 mL 0.5863 mL 1.4657 mL
    80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
    100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 mL
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    • 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.

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