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KNK437 inhibit stress-induced synthesis of heat shock proteins (HSPs). 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).
In vivo, KNK437 (62.5-400 mg/kg) recovers bodyweight losses of tumor-free CD-1 (ICR) mice. KNK437 (200 mg/kg) alone shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors.
Environ Res. 2025 Feb 17;1:272:121151.
Modulated regulation of the stress-feeding-growth neuroendocrine cascade in Chinese sea bass (Lateolabrax maculatus) under temperature and salinity changes
KNK437 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | COLO 320DM cells |
| Preparation method | 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. |
| Concentrations | 0, 25, 50, 100, 150, and 200 μm |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | tumor-free CD-1 (ICR) mice |
| Formulation | dissolved in olive oil |
| Dosages | 62.5 to 500 mg/kg |
| Administration | i.p. |
| Molecular Weight | 245.23 |
| Formula | C13H11NO4 |
| CAS Number | 218924-25-5 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HSP Products |
|---|
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| CUDC-305
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| Ganetespib
Ganetespib (STA-9090) is a potent synthetic small molecule inhibitor of Hsp90 with potential antineoplastic activity. |
| Luminespib (AUY922)
Luminespib (AUY922) is a small molecule Heat Shock Protein 90 (HSP90) inhibitor with IC50 values of 13 and 21 nM for HSP90α and HSP90β respectively. |
| NVP-HSP990
NVP-HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively. NVP-HSP990 has potential antineoplastic activity. |
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