KRIBB11
Based on 20 publication(s) in Google Scholar
KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.69%
- No. CAS: 342639-96-7
- Fòrmula: C13H12N6O2
- Peso molecular:284.27
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) KRIBB11
More- Cancer Res. 2019 Oct 15;79(20):5233-5244. [Abstract]
- Sci Transl Med. 2020 May 6;12(542):eaba0769. [Abstract]
- J Exp Clin Cancer Res. 2024 Sep 6;43(1):253. [Abstract]
- J Exp Clin Cancer Res. 2021 Jan 9;40(1):25. [Abstract]
- Cell Death Dis. 2017 Dec 12;8(12):3203. [Abstract]
- Acta Pharmacol Sin. 2022 Oct;43(10):2550-2561. [Abstract]
- EMBO Mol Med. 2021 Aug 9;13(8):e13792. [Abstract]
- Biochem Pharmacol. 2024 May:223:116155. [Abstract]
- Mol Cancer Res. 2020 Mar;18(3):463-476. [Abstract]
- Reprod Biol Endocrinol. 2021 Jun 9;19(1):86. [Abstract]
- Sci Rep. 2025 Aug 13;15(1):29741. [Abstract]
- Sci Rep. 2024 Apr 8;14(1):8241. [Abstract]
- Mol Oncol. 2017 Oct;11(10):1475-1492. [Abstract]
- J Proteome Res. 2023 Sep 1;22(9):2880-2889. [Abstract]
- Arch Biochem Biophys. 2023 Mar 1:736:109525. [Abstract]
- Am J Cancer Res. 2024 May 15;14(5):2072-2087. [Abstract]
- Environ Toxicol. 2024 Jan;39(1):9-22. [Abstract]
- Biomed Pharmacother. 2022 Apr:148:112713. [Abstract]
- bioRxiv. January 21, 2022.
- Patent. US20210380988A1.
Customer Validation & Images
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IHC
Actividad biológica
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HSF1 1.2 μM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 342639-96-7
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Appearance Solid
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Peso molecular 284.27
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Fòrmula C13H12N6O2
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Color Yellow to orange
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SMILES
CNC1=CC=C([N+]([O-])=O)C(NC2=CC3=C(NN=C3)C=C2)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (20)
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Journal Impact Factor
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Most Recent
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Cancer Res
Phosphorylation of HSF1 by PIM2 Induces PD-L1 Expression and Promotes Tumor Growth in Breast Cancer. [Abstract]2019 Oct 15;79(20):5233-5244. PMID: 31409638 -
Sci Transl Med
2020 May 6;12(542):eaba0769. PMID: 32376767 -
J Exp Clin Cancer Res
HSF1 is a prognostic determinant and therapeutic target in intrahepatic cholangiocarcinoma. [Abstract]2024 Sep 6;43(1):253. PMID: 39243039 -
J Exp Clin Cancer Res
2021 Jan 9;40(1):25. PMID: 33422093 -
Cell Death Dis
Receptor-interacting protein 140 as a co-repressor of Heat Shock Factor 1 regulates neuronal stress response. [Abstract]2017 Dec 12;8(12):3203. PMID: 29233969
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.
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Acta Pharmacol Sin
Trimetazidine enhances myocardial angiogenesis in pressure overload-induced cardiac hypertrophy mice through directly activating Akt and promoting the binding of HSF1 to VEGF-A promoter. [Abstract]2022 Oct;43(10):2550-2561. PMID: 35217815 -
EMBO Mol Med
2021 Aug 9;13(8):e13792. PMID: 34223704 -
Biochem Pharmacol
Suppression of NSCLC progression via the co-administration of Danusertib, an AURK inhibitor, and KRIBB11, an HSF1 inhibitor. [Abstract]2024 May:223:116155. PMID: 38521474 -
Mol Cancer Res
HSF1-Mediated Control of Cellular Energy Metabolism and mTORC1 Activation Drive Acute T-Cell Lymphoblastic Leukemia Progression. [Abstract]2020 Mar;18(3):463-476. PMID: 31744878 -
Reprod Biol Endocrinol
HSF1 promotes endometriosis development and glycolysis by up-regulating PFKFB3 expression. [Abstract]2021 Jun 9;19(1):86. PMID: 34107992 -
Sci Rep
HSF1 in macrophages suppressed the progression of asthma via modulating SIRPα/SHP2-Dectin-1/ SYK mediated ROS and inflammatory responses. [Abstract]2025 Aug 13;15(1):29741. PMID: 40804251 -
Sci Rep
Heat shock factor 1 inhibition enhances the effects of modulated electro hyperthermia in a triple negative breast cancer mouse model. [Abstract]2024 Apr 8;14(1):8241. PMID: 38589452 -
Mol Oncol
Loss of AMPK activation promotes the invasion and metastasis of pancreatic cancer through an HSF1-dependent pathway. [Abstract]2017 Oct;11(10):1475-1492. PMID: 28783244
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.
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J Proteome Res
Quantitative Proteomics of the CDK9 Interactome Reveals a Function of the HSP90-CDC37-P-TEFb Complex for BETi-Induced HIV-1 Latency Reactivation. [Abstract]2023 Sep 1;22(9):2880-2889. PMID: 37540094 -
Arch Biochem Biophys
N-butyrate increases heat shock protein 70 through heat shock factor 1 and AMP-activated protein kinase pathways in human intestinal Caco-2 cells. [Abstract]2023 Mar 1:736:109525. PMID: 36702450
KRIBB11 purchased from MedChemExpress. Usage Cited in: Arch Biochem Biophys. 2023 Mar 1:736:109525. [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).
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Am J Cancer Res
The small-molecule drug homoharringtonine targets HSF1 to suppress pancreatic cancer progression. [Abstract]2024 May 15;14(5):2072-2087. PMID: 38859866 -
Environ Toxicol
MUC1 promotes lymph node metastasis in esophageal squamous cell carcinoma by downregulating DNAJB6 expression. [Abstract]2024 Jan;39(1):9-22. PMID: 37584547 -
Biomed Pharmacother
Heat shock factor 1 inhibition sensitizes pancreatic cancer to gemcitabine via the suppression of cancer stem cell-like properties. [Abstract]2022 Apr:148:112713. PMID: 35158144 -
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Solvente y solubilidad
DMSO : 150 mg/mL (527.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yoon YJ, et al. KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to the hsp70 promoter. J Biol Chem. 2011 Jan 21;286(3):1737-47 [Content Brief]
[2]. Samarasinghe B, et al. Heat shock factor 1 confers resistance to Hsp90 inhibitors through p62/SQSTM1 expression and promotion of autophagic flux. Biochem Pharmacol. 2014 Feb 1;87(3):445-55 [Content Brief]
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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