1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP

KRIBB11 

Cat. No.: HY-100872 Purity: 99.04%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 216 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 648 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    KRIBB11 purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Dec 12;8(12):3203.

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

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.3518 mL 1.7589 mL 3.5178 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    KRIBB11 is dissolved in 10% dimethylacetamide, 50% PEG300, and 40% distilled water.

    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
    Molecular Weight

    284.27

    Formula

    C₁₃H₁₂N₆O₂

    CAS No.

    342639-96-7

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 27 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    KRIBB11
    Cat. No.:
    HY-100872
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