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KNK437

Cat. No. M9304
KNK437 Structure
Synonym:

Heat Shock Protein Inhibitor I

Size Price Availability Quantity
10mg USD 95  USD95 In stock
50mg USD 333  USD333 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Koishi M, et al. Clin Cancer Res. The effects of KNK437, a novel inhibitor of heat shock protein synthesis, on the acquisition of thermotolerance in a murine transplantable tumor in vivo.

[2] Yokota S, et al. Cancer Res. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells.

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Keywords: KNK437, Heat Shock Protein Inhibitor I supplier, HSP, inhibitors, activators


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