KNK437
Based on 7 publication(s) in Google Scholar
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 218924-25-5
- Formula: C13H11NO4
- Molecular Weight:245.23
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KNK437
More- ACS Nano. 2025 Aug 19;19(32):29073-29086. [Abstract]
- Nat Commun. 2023 Jul 26;14(1):4505. [Abstract]
- MedComm (2020). 2025 Mar 10;6(3):e70129. [Abstract]
- Ecotoxicol Environ Saf. 2025 Apr 4:295:118137. [Abstract]
- Int J Mol Sci. 2025 Oct 13;26(20):9963. [Abstract]
- Fish Shellfish Immunol. 2017 Nov;70:185-194. [Abstract]
- Viruses. 2025 Jul 22;17(8):1025. [Abstract]
Customer Validation & Images
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RT-PCR
Biological Activity
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HSP105 |
HSP70 |
HSP40 |
KNK437 inhibits the activation of several HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells. KNK437 (100 μM) inhibits thermotolerance in COLO 320DM cells after the first heat treatment. KNK437 shows inhibitory effects on thermotolerance dose-dependently in COLO 320DM cells (0-200 μM) and HeLa S3 cells (100, 200 μM)[1]. KNK437 (100 μM) exhibits inhibitory activities against the methylation of H3-Lys4 before or after heat-treatment in HSC4 cells and KB cells, but does not affect that of H3 Lys9. KNK437 also suppresses the expression of HSP70[3].
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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CAS No. 218924-25-5
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Appearance Solid
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Molecular Weight 245.23
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Formula C13H11NO4
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Color Light yellow to yellow
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SMILES
O=CN1C(/C(CC1)=C/C2=CC=C(OCO3)C3=C2)=O
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Synonyms
Heat Shock Protein Inhibitor I
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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ACS Nano
Quantitative and Reversible Regulation of Yes-Associated Protein Activity by Ultrasmall Nanoparticle-Mediated Magnetothermal Stimulation of F-Actin. [Abstract]2025 Aug 19;19(32):29073-29086. PMID: 40763353 -
Nat Commun
Generation of whole tumor cell vaccine for on-demand manipulation of immune responses against cancer under near-infrared laser irradiation. [Abstract]2023 Jul 26;14(1):4505. PMID: 37495590 -
MedComm (2020)
Heat Shock Protein Family A Member 1A Attenuates Apoptosis and Oxidative Stress via ERK/JNK Pathway in Hyperplastic Prostate. [Abstract]2025 Mar 10;6(3):e70129. PMID: 40066224 -
Ecotoxicol Environ Saf
Maternal exposure to Aristolochic Acid I affects meiotic I progression by impairing DNA damage repair in fetal oocytes. [Abstract]2025 Apr 4:295:118137. PMID: 40187211 -
Int J Mol Sci
HSP90 Inhibition Disrupts 27-Hydroxycholesterol-Induced Inflammatory Signaling in Monocytic Cells. [Abstract]2025 Oct 13;26(20):9963. PMID: 41155259 -
Fish Shellfish Immunol
The antiviral role of heat shock protein 27 against red spotted grouper nervous necrosis virus infection in sea perch. [Abstract]2017 Nov;70:185-194. PMID: 28860076
KNK437 purchased from MedChemExpress. Usage Cited in: Fish Shellfish Immunol. 2017 Nov;70:185-194. [Abstract]
Treatment with KNK437, an antagonist of HSP27, leads to significant up-regulation of RDRP at 24 and 48 hpi.
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Viruses
DNAJ Homolog Subfamily C Member 11 Stabilizes SARS-CoV-2 NSP3 to Promote Double-Membrane Vesicle Formation. [Abstract]2025 Jul 22;17(8):1025. PMID: 40872740
Solvent & Solubility
DMSO : 10 mg/mL (40.78 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (40.78 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 10 mg/mL (40.78 mM); Suspended solution; Need ultrasonic
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.
Protocol
Heat treatments at 42°C for 90 min are performed in a CO2 incubator using 25-cm2 plastic flasks. Cells (1 × 105) are seeded in the flasks, incubated at 37°C for 48 h, and then heated by immersing the flasks in a water bath (45°C ± 0.05°C). KNK437 and quercetin are dissolved in DMSO before being added at the indicated concentrations. The final concentration of DMSO in each culture medium is 0.25% (v/v), irrespective of the concentrations of the drugs. The same concentration of DMSO is used as a control. Sodium arsenite is dissolved in PBS at a concentration of 80 mM and added to the medium. Cells are treated with 300 μM sodium arsenite at 37°C for 1.5 h, rinsed, and then incubated at 37°C for 5 h before 45°C heat challenge[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To subject the tumors to hyperthermia, the right foot of each mouse is immersed in a water bath maintained at the desired temperature to an accuracy of ± 0.05°C. After the mouse has been anesthetized with 50 mg/kg pentobarbital sodium solution, the tumor-bearing leg is pulled down into the water bath using a special sinker (weighing ∼45 g) taped to the skin of the toe. Care is taken not to impair the blood flow in the limb. While the extended right leg is receiving local heat, the mouse is air-cooled. KNK437 is dissolved in olive oil immediately before use. The KNK437 is administered i.p. 6 h before the first heat treatment. It is used mainly at a concentration of 200 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yokota S, et al. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells. Cancer Res. 2000 Jun 1;60(11):2942-8. [Content Brief]
[2]. Koishi M, et al. The effects of KNK437, a novel inhibitor of heat shock protein synthesis, on the acquisition of thermotolerance in a murine transplantable tumor in vivo. Clin Cancer Res. 2001 Jan;7(1):215-9. [Content Brief]
[3]. Matsuda K, et al. Effects of KNK437 on heat-induced methylation of histone H3 in human oral squamous cell carcinoma cells. Int J Hyperthermia. 2006 Dec;22(8):729-35. [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 |
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| DMSO | 1 mM | 4.0778 mL | 20.3890 mL | 40.7780 mL | 101.9451 mL |
| 5 mM | 0.8156 mL | 4.0778 mL | 8.1556 mL | 20.3890 mL | |
| 10 mM | 0.4078 mL | 2.0389 mL | 4.0778 mL | 10.1945 mL | |
| 15 mM | 0.2719 mL | 1.3593 mL | 2.7185 mL | 6.7963 mL | |
| 20 mM | 0.2039 mL | 1.0195 mL | 2.0389 mL | 5.0973 mL | |
| 25 mM | 0.1631 mL | 0.8156 mL | 1.6311 mL | 4.0778 mL | |
| 30 mM | 0.1359 mL | 0.6796 mL | 1.3593 mL | 3.3982 mL | |
| 40 mM | 0.1019 mL | 0.5097 mL | 1.0195 mL | 2.5486 mL |
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