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KNK437

Catalog No. T2444 CAS 218924-25-5

Synonyms: Heat Shock Protein Inhibitor I

KNK437 (Heat Shock Protein Inhibitor I), a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40).

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KNK437, CAS 218924-25-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 161.00
50 mg	In stock	$ 292.00
100 mg	In stock	$ 549.00
200 mg	In stock	$ 756.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 98%

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Description	KNK437 (Heat Shock Protein Inhibitor I), a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40).
In vivo	KNK437 (200 mg/kg, i.p.) shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors. The same dose of KNK437 enhances the antitumor effects of fractionated heat treatment in a synergistic manner.[3]
Kinase Assay	Metabolic Labeling and Gel Electrophoresis: COLO 320DM cells (200,000) are injected into each well of 12-well plastic plates 2 days before incubation in the presence of KNK437 for 1 h before heat shock. The cells are then heat-shocked at 42°C for 90 min or kept at 37°C for the same length of time and incubated at 37°C for 2 h. For metabolic labeling, cells are washed with PBS without Ca2+ or Mg2+ and incubated for 1 h with 1.22 MBq of [35S]methionine in 250 μL of methionine-free DMEM supplemented with 10% dialyzed fetal bovine serum. After metabolic labeling, cells are washed twice with PBS and lysed in a buffer containing 1% NP40, 0.15 M NaCl, 50 mM Tris-HCl (pH 8.0), 5 mM EDTA, and protease inhibitors [0.2 mM 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride, 2 mM N-ethylmaleimide, 1 μg/mL pepstatin, and 1 μg/mL leupeptin]. After centrifugation at 12,000×g for 20 min, cell extracts containing equal amounts of trichloroacetic acid-insoluble radioactivity are analyzed by two-dimensional gel electrophoresis (the one-dimensional gel electrophoresis is a nonequilibrium pH gradient gel electrophoresis, and the two-dimensional gel electrophoresis is 10% SDS-PAGE).
Cell Research	Thermotolerance is induced by incubating cells with 300 μM sodium arsenite for 90 min. Cells are preincubated with or without 100 μM KNK437 for 1 h before the sodium arsenite treatment. After treatment of the cells with sodium arsenite, cells are washed once with PBS and incubated at 37℃ for 5 h with or without KNK437. The effects of KNK437 on acquired thermotolerance are tested by heating the cells at 45°C for the indicated time. The surviving fraction is calculated as the plating efficiency of the treated cells divided by the plating efficiency of untreated control cells.(Only for Reference)

Synonyms	Heat Shock Protein Inhibitor I
Molecular Weight	245.23
Formula	C13H11NO4
CAS No.	218924-25-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 12 mg/mL (48.9 mM)

References and Literature

1. Yokota S, et al. Cancer Res. 2000, 60(11), 2942-2948. 2. Sahin E, et al. Int J Hyperthermia. 2011, 27(1), 63-73. 3. Koishi M, et al. Clin Cancer Res. 2001, 7(1), 215-219.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Anti-Breast Cancer Compound Library Anti-Aging Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compounds Library Max Preclinical Compound Library Metabolism Compound Library NO PAINS Compound Library

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Keywords

KNK437 218924-25-5 Cytoskeletal Signaling Metabolism HSP KNK-437 inhibit Heat shock proteins KNK 437 Heat Shock Protein Inhibitor I Inhibitor inhibitor

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