KRIBB11 |
Catalog No.GC19215
One-Click Copy Product Info
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KRIBB11 is a potent heat shock factor 1 (HSF1) inhibitor, with an IC50 value of 1.2µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 342639-96-7
Sample solution is provided at 25 µL, 10mM.
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KRIBB11 is a potent heat shock factor 1 (HSF1) inhibitor, with an IC50 value of 1.2µM[1]. KRIBB11 promotes the proteasomal degradation of Mcl-1 by mediating the ubiquitination increase through the E3 ubiquitin ligase Mule, thereby exerting an apoptotic effect[2]. KRIBB11 has been widely used to promote microglial process elongation and suppress neuroinflammation[3].
In vitro, KRIBB11 treatment for 48 hours significantly inhibited the viability of MCF-7, BT-474, and BT-20 cells, with IC50 values of 3µM, 25µM, and 16µM, respectively [4]. Treatment with 12.5µM KRIBB11 for 24h induced DNA damage, upregulated p53 and p21, and reduced the expression of cyclin D2/E, CDK2/4, c-Myc, MDM2, and β-catenin in human T-cell leukemia virus type 1 (HTLV-1)-infected T cells[5]. 5µM of KRIBB11 incubation for 48 hours significantly promoted apoptosis of A172 cells, accompanied by accumulation of p53 and decrease in p27 levels[6].
In vivo, a single intraperitoneal injection of KRIBB11 (5mg/kg) 1 hour before lipopolysaccharide (LPS) injection suppressed the expression of iNOS protein and mRNA in the brain tissue of endotoxemic mice[7]. Intraperitoneal injection of KRIBB11 at a dose of 50mg/kg/day for 8 consecutive days, combined with 4 sessions of Modulated electro-hyperthermia (mEHT), inhibited tumor growth in the 4T1 xenograft mouse model[8]. Continuous intraperitoneal injection of KRIBB11 (50mg/kg/day) for 30 consecutive days delayed the occurrence of pancreatic cancer in LSL-KrasG12D/+; Pdx1-Cre mice and inhibited the formation of pancreatic cancer precancerous lesions induced by pancreatitis[9].
References:[1]Yoon Y J, Kim J A, Shin K D, 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]. Journal of Biological Chemistry, 2011, 286(3): 1737-1747.
[2] Kang M J, Yun H H, Lee J H. KRIBB11 accelerates Mcl-1 degradation through an HSF1-independent, Mule-dependent pathway in A549 non-small cell lung cancer cells[J]. Biochemical and biophysical research communications, 2017, 492(3): 304-309.
[3] Su J, Dou Z, Hong H, et al. KRIBB11: A promising drug that promotes microglial process elongation and suppresses neuroinflammation[J]. Frontiers in Pharmacology, 2022, 13: 857081.
[4] Carpenter R L, Sirkisoon S, Zhu D, et al. Combined inhibition of AKT and HSF1 suppresses breast cancer stem cells and tumor growth[J]. Oncotarget, 2017, 8(43): 73947.
[5] Ishikawa C, Mori N. Heat shock factor 1 is a promising therapeutic target against adult T-cell leukemia[J]. Medical Oncology, 2023, 40(6): 172.
[6] Yoo K, Yun H H, Jung S Y, et al. KRIBB11 Exerts Anticancer Effects on A172 Glioblastoma Cells via the Cdh1/SKP2/p27 and HSF1/p53/p21 Pathways[J]. Cancer Genomics-Proteomics, 2025, 22(3): 467-477.
[7] Huang C, Lu X, Tong L, et al. Requirement for endogenous heat shock factor 1 in inducible nitric oxide synthase induction in murine microglia[J]. Journal of Neuroinflammation, 2015, 12(1): 189.
[8] Viana P H L, Schvarcz C A, Danics L O, et al. Heat shock factor 1 inhibition enhances the effects of modulated electro hyperthermia in a triple negative breast cancer mouse model[J]. Scientific Reports, 2024, 14(1): 8241.
[9] Qian W, Chen K, Qin T, et al. The EGFR-HSF1 axis accelerates the tumorigenesis of pancreatic cancer[J]. Journal of Experimental & Clinical Cancer Research, 2021, 40(1): 25.
| Cell experiment [1]: | |
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Cell lines |
A549 cells |
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Preparation Method |
A549 cells were cultured in RPMI 1640 medium, supplemented 1% penicillin-streptomycin and 10% fetal bovine serum (FBS), in a humidified 5% CO2 incubator at 37°C. Cells were seeded at a density of 5×103 cells per well into 96-well plates 24h. A549 cells were exposed to varying concentrations of KRIBB11 (0, 0.01, 0.05, 0.1, 0.5, 1, 5, 10, 25, and 50μM, respectively). After 24h of treatment, cell viability was calculated. |
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Reaction Conditions |
0, 0.01, 0.05, 0.1, 0.5, 1, 5, 10, 25, and 50μM; 24h |
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Applications |
KRIBB11 treatment reduced cell viability of A549 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
LSL-KrasG12D/+; Pdx1-Cre mice |
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Preparation Method |
LSL-KrasG12D/+; Pdx1-Cre mice (8 weeks of age) were fed ad libitum under controlled light-dark cycles (12h of light followed by 12h of dark) at 22±3°C. Mice were treated with KRIBB11 (50mg/kg/day; i.p.) for 1 month. After euthanasia, mouse pancreatic tissues were harvested for analysis. |
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Dosage form |
50mg/kg/day; 1 month; i.p. |
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Applications |
KRIBB11 treatment suppressed tumorigenesis of pancreatic cancer in LSL-KrasG12D/+; Pdx1-Cre mice. |
| References: [1] Zhang X, Lei Y, Chen X, et al. Suppression of NSCLC progression via the co-administration of Danusertib, an AURK inhibitor, and KRIBB11, an HSF1 inhibitor[J]. Biochemical Pharmacology, 2024, 223: 116155. [2] Qian W, Chen K, Qin T, et al. The EGFR-HSF1 axis accelerates the tumorigenesis of pancreatic cancer[J]. Journal of Experimental & Clinical Cancer Research, 2021, 40(1): 25. | |
| Cas No. | 342639-96-7 | SDF | |
| Canonical SMILES | CNC1=CC=C([N+]([O-])=O)C(NC2=CC3=C(NN=C3)C=C2)=N1 | ||
| Formula | C13H12N6O2 | M.Wt | 284.27 |
| Solubility | DMSO : ≥ 27 mg/mL (94.98 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5178 mL | 17.5889 mL | 35.1778 mL |
| 5 mM | 703.6 μL | 3.5178 mL | 7.0356 mL |
| 10 mM | 351.8 μL | 1.7589 mL | 3.5178 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)