KNK437 (Synonyms: Hsp Inhibitor I, KNK 437) |
カタログ番号GC11930
One-Click Copy Product Info
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KNK437 は HSP 阻害剤であり、HSP105、HSP70、および HSP40 の誘導を阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 218924-25-5
Sample solution is provided at 25 µL, 10mM.
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KNK437 is a benzylidene lactam compound that inhibits stress-induced HSPs (heat shock proteins) synthesis.
HSPs (heat shock proteins) are chaperones that their expressions are increased under various cellular stresses including temperature rise. It plays a vital role in regulating protein folding and associated with cancer and cardiovascular diseases.
KNK437 inhibits the acquisition of thermotolerance and the induction of various HSPs in human colon carcinoma cells (COLO 320DM) in a dose-dependent manner. KNK437 also blocks the acquisition of thermotolerance that developed by sodium arsenite. [1]
KNK437 exerts low toxicity in vivo. In C3H/He mice transplanted with SCC VII cells, the concentration of KNK437 in the tumors gradually increases and reaches a peak 6 hours after i.p. injection. Hsp72 were synthesized 8 h after hyperthermia at 44 oC for 10 minutes, and their synthesis is inhibited by administration of KNK437 6 hours before hyperthermia. [2]
References:
1. Yokota S, Kitahara M, Nagata K. 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.
2. Koishi M, Yokota S, Mae T 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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
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. | |
| Cas No. | 218924-25-5 | SDF | |
| 同義語 | Hsp Inhibitor I, KNK 437 | ||
| Chemical Name | (E)-3-(benzo[d][1,3]dioxol-5-ylmethylene)-2-oxopyrrolidine-1-carbaldehyde | ||
| Canonical SMILES | O=CN1C(/C(CC1)=C/C2=CC=C(OCO3)C3=C2)=O | ||
| Formula | C13H11NO4 | M.Wt | 245.23 |
| 溶解度 | ≥ 12.25mg/mL in DMSO with ultrasonic | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.0778 mL | 20.389 mL | 40.778 mL |
| 5 mM | 815.6 μL | 4.0778 mL | 8.1556 mL |
| 10 mM | 407.8 μL | 2.0389 mL | 4.0778 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 27 reference(s) in Google Scholar.)