ChemicalBook > CAS DataBase List > KNK437

KNK437

Product Name
KNK437
CAS No.
218924-25-5
Chemical Name
KNK437
Synonyms
KNK437;KNK423;CS-1681;KNK-437;KNK 437;HEAT SHOCK PROTEIN INHIBITOR I;HEAT SHOCK PROTEIN INHIBITOR II;KNK 437 (Heat Shock Protein Inhibitor I);3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM;N-Formyl-3,4-methylenedioxy-benzylidene-g-butyrolactam;N-FORMYL-3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM
CBNumber
CB4713272
Molecular Formula
C13H11NO4
Formula Weight
245.23
MOL File
Mol file
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KNK437 Property

Boiling point:
412.4±55.0 °C(Predicted)
Density 
1.515±0.06 g/cm3(Predicted)
storage temp. 
room temp
solubility 
DMSO: soluble5mg/mL, clear (warmed)
form 
White to light yellow powder
pka
-1.70±0.20(Predicted)
color 
white to beige
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0964
Product name
KNK437
Purity
≥98% (HPLC)
Packaging
5mg
Price
$118
Updated
2024/03/01
Sigma-Aldrich
Product number
373260
Product name
Heat Shock Protein Inhibitor I
Packaging
5mg
Price
$216
Updated
2024/03/01
Cayman Chemical
Product number
15395
Product name
Heat Shock Protein Inhibitor I
Purity
≥98%
Packaging
1mg
Price
$47
Updated
2024/03/01
Cayman Chemical
Product number
15395
Product name
Heat Shock Protein Inhibitor I
Purity
≥98%
Packaging
5mg
Price
$92
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0964
Product name
KNK437
Purity
≥98% (HPLC)
Packaging
25mg
Price
$478
Updated
2024/03/01
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KNK437 Chemical Properties,Usage,Production

Description

KNK437 (218924-25-5) Inhibits constitutive and inducible HSP70 expression in non-stressed1 and heat-stressed2 cancer cells. Blocks the geldanamycin-induced induction of HSP70 and inhibition of TGF? signaling.3 Inhibits leukocyte integrin α4?7-mediated adhesion of T cells to mucosal addressin cell adhesion molecule 1 (MAdCAM-1) suggesting that HSP70 is essential for ?7 integrin signalling.4 Suppresses morphine analgesic tolerance in a rodent model (100 mg/Kg).5

Uses

KNK437 has been used:

  • as a heat shock factor 1 (HSF1) inhibitor to study its effects on the inhibition of viability and apoptosis activation in chemoresistant mice cells
  • as an HSF1 inhibitor to study its effects on viability and apoptosis of colorectal cancer cells
  • as a heat shock protein 70 (HSP70) inhibitor to study its effects on glutamine-induced HSP70 and inflammatory mediator release

Biological Activity

KNK437 is a pan-HSP inhibitor that inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.

Biochem/physiol Actions

KNK437 inhibits the accumulation of heat shock proteins (including hsp -27, -40, -70, -72 and -105). KNK437 inhibits thermotolerance in cells with greater potency than quercetin.

in vitro

In COLO320DM (human colon cancer) cells, KNK437 dose-dependently inhibits acquisition of thermotolerance and the activity of various HSPs, including Hsp105, HSP70 and HSP40. In PC-3 cells, KNK437 and quercetin dose-dependently inhibited thermotolerance. In PC-3 and LNCaP cells, KNK437 reduced heat-induced accumulation of HSP70 mRNA and protein.

in vivo

KNK437 (200 mg/kg, intraperitoneal injection) showed no antitumor effect and did not increase the thermosensitivity of non-tolerant tumors. The same dose of KNK437 can synergistically improve the antitumor efficacy of graded heat treatment.

References

Shiota et al. (2010), Heat shock cognate protein 70 is essential for Akt signaling in endothelial function; Thromb. Vasc. Biol., 30 491 Yokota et al. (2000), Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells; Cancer Res., 60 2942 Yun et al. (2010), Geldanamycin inhibits TGF-beta signaling through induction of Hsp70; Biochem. Biophys., 495 8 Chan et al. (2015), Leukocyte integrin α4?7 associates with heat shock protein 70; Cell. Biochem., 409 263 Qin et al. (2020), Effect of heat chock protein 70 modulators on the development of morphine analgesic tolerance in rats; Pharmacol., 31 179

KNK437 Preparation Products And Raw materials

Raw materials

Preparation Products

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KNK437 Suppliers

China 61 India 1 United Kingdom 1 United States 15 Global 78
Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
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View Lastest Price from KNK437 manufacturers

Career Henan Chemical Co
Product
3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM 218924-25-5
Price
US $1.00/KG
Min. Order
1KG
Purity
98-100%
Supply Ability
1000kg
Release date
2018-08-20

218924-25-5, KNK437Related Search:

Levetiracetam N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Dequalinium chloride Acalabrutinib

  • N-FORMYL-3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM
  • 3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM
  • KNK423
  • KNK437
  • HEAT SHOCK PROTEIN INHIBITOR I
  • HEAT SHOCK PROTEIN INHIBITOR II
  • 3-(1,3-Benzodioxol-5-ylmethylene)-2-oxo-1-pyrrolidinecarboxaldehyde
  • Heat Shock Protein Inhibitor I - CAS 218924-25-5 - Calbiochem
  • CS-1681
  • 3-[(E)-1,3-Benzodioxol-5-ylmethylene]-2-oxopyrrolidine-1-carbaldehyde
  • KNK-437;KNK 437
  • 1-Pyrrolidinecarboxaldehyde, 3-(1,3-benzodioxol-5-ylmethylene)-2-oxo-
  • N-Formyl-3,4-methylenedioxy-benzylidene-g-butyrolactam
  • 3-(Benzo[d][1,3]dioxol-5-ylmethylene)-2-oxopyrrolidine-1-carbaldehyde
  • HSP,inhibit,Heat shock proteins,KNK-437,KNK437,KNK 437,Inhibitor
  • KNK 437 (Heat Shock Protein Inhibitor I)
  • 218924-25-5
  • API
  • Inhibitors