KNK437
Inhibits HSP70 expression / Inhibits constitutive and inducible HSP70 expression in non-stressed1 and heat-stressed2 cancer cells. Blocks the geldanamycin-induced induction of HSP70 and inhibition of TGFß signaling.3 Inhibits leukocyte integrin α4ß7-mediated adhesion of T cells to mucosal addressin cell adhesion molecule 1 (MAdCAM-1) suggesting that HSP70 is essential for ß7 integrin signalling.4 Suppresses morphine analgesic tolerance in a rodent model (100 mg/Kg).5
Biochemicals & reagents
218924-25-5
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 α4ß7 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
-20°C
TARGET: HSP (Heat shock protein) -- PATHWAY: Cell adhesion -- DISEASE AREA: Cancer; Pain