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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
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 245.23
Formula C13H11NO4
CAS Number 218924-25-5
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
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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  Catalog
Abmole Inhibitor Catalog 2017




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

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