KNK437
- Product Name
- KNK437
- CAS No.
- 218924-25-5
- Chemical Name
- KNK437
- Synonyms
- KNK437;KNK423;CS-1681;KNK-437;KNK 437;KNK437, 10 mM in DMSO;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
- CBNumber
- CB4713272
- Molecular Formula
- C13H11NO4
- Formula Weight
- 245.23
- MOL File
- Mol file
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.
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0964
- Product name
- KNK437
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $121
- Updated
- 2025/07/31
- Product number
- 373260
- Product name
- Heat Shock Protein Inhibitor I
- Packaging
- 5mg
- Price
- $189
- Updated
- 2025/07/31
- Product number
- 15395
- Product name
- Heat Shock Protein Inhibitor I
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $47
- Updated
- 2024/03/01
- Product number
- 15395
- Product name
- Heat Shock Protein Inhibitor I
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $92
- Updated
- 2024/03/01
- Product number
- SML0964
- Product name
- KNK437
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $491
- Updated
- 2025/07/31
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
[1] MASAYUKI SHIOTA. Heat shock cognate protein 70 is essential for Akt signaling in endothelial function.[J]. Arteriosclerosis, Thrombosis, and Vascular Biology, 2010, 30 3: 491-497. DOI:10.1161/atvbaha.109.193631
[2] S YOKOTA K N M Kitahara. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells.[J]. Cancer research, 2000, 60 11: 2942-2948.
[3] CHANG-HYUN YUN . Geldanamycin inhibits TGF-β signaling through induction of Hsp70[J]. Archives of biochemistry and biophysics, 2010, 495 1: Pages 8-13. DOI:10.1016/j.abb.2009.12.003
[4] Leukocyte integrin α4?7 associates with heat shock protein 70
[5] WANGJUN QIN. Effect of heat shock protein 70 modulators on the development of morphine analgesic tolerance in rats[J]. Behavioural Pharmacology, 2019, 31 1: 179-185. DOI:10.1097/fbp.0000000000000528
KNK437 Preparation Products And Raw materials
Raw materials
Preparation Products
KNK437 Suppliers
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- 50966098
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View Lastest Price from KNK437 manufacturers
- 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