KNK437

ChemicalBook > CAS DataBase List > 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

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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