KNK437 (Synonyms: Heat Shock Protein Inhibitor I)

Name: KNK437
Brand: MedChemExpress
SKU: HY-100110
Rating: 5.0 (3 reviews)

Cat. No.: HY-100110 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

For research use only. We do not sell to patients.

KNK437 Chemical Structure

CAS No. : 218924-25-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 686	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 924	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE KNK437

RT-PCR

: 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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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

IC₅₀ & Target^[1]

HSP105

HSP70

HSP40

In Vitro

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.

In Vivo

KNK437 is a weakly toxic agent. 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. KNK437 improves the antitumor effects of fractionated heat treatment at 44°C at 200 mg/kg in a synergistic manner. KNK437 (200 mg/kg, i.p.) suppresses the induction of thermotolerance when administrated 6 h before the initial heating^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

245.23

Formula

C₁₃H₁₁NO₄

CAS No.

218924-25-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=CN1C(/C(CC1)=C/C2=CC=C(OCO3)C3=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0778 mL	20.3890 mL	40.7780 mL
5 mM	0.8156 mL	4.0778 mL	8.1556 mL
10 mM	0.4078 mL	2.0389 mL	4.0778 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 1 mg/mL (4.08 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 1 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (40.78 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 10 mg/mL (40.78 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) HNMR (244 KB)

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]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

KNK437 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KNK437218924-25-5Heat Shock Protein Inhibitor IKNK 437KNK-437HSPHeat shock proteinsInhibitorinhibitorinhibit

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KNK437 (Synonyms: Heat Shock Protein Inhibitor I)

Customer Review

KNK437 Related Antibodies

2 Publications Citing Use of MCE KNK437

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•Related Screening Libraries:

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View All HSP Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

KNK437 Related Antibodies

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Complete Stock Solution Preparation Table

KNK437 Related Classifications

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