KNK437 Struktur

KNK437

Bezeichnung:KNK437

CAS-Nr218924-25-5

Englisch Name:KNK437

CBNumberCB4713272

SummenformelC13H11NO4

Molgewicht245.23

MOL-DateiMol file

KNK437 physikalisch-chemischer Eigenschaften

Siedepunkt	412.4±55.0 °C(Predicted)
Dichte	1.515±0.06 g/cm3(Predicted)
storage temp.	room temp
Löslichkeit	DMSO: soluble5mg/mL, clear (warmed)
Aggregatzustand	White to light yellow powder
pka	-1.70±0.20(Predicted)
Farbe	white to beige
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

WGK Germany

KNK437 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Verwenden
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
Biologische Aktivität
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.
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

218924-25-5, KNK437 Verwandte Suche:

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