218924-25-5KNK437

产品属性：

Cas No.218924-25-5

别名 N/A

化学名 (E)-3-(benzo[d][1,3]dioxol-5-ylmethylene)-2-oxopyrrolidine-1-carbaldehyde

分子式 C13H11NO4

分子量 245.23

溶解度 ≥ 12.25mg/mL in DMSO with ultrasonic

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
KNK437 is a benzylidene lactam compound that inhibits stress-induced HSPs (heat shock proteins) synthesis.

HSPs (heat shock proteins) are chaperones that their expressions are increased under various cellular stresses including temperature rise. It plays a vital role in regulating protein folding and associated with cancer and cardiovascular diseases.

KNK437 inhibits the acquisition of thermotolerance and the induction of various HSPs in human colon carcinoma cells (COLO 320DM) in a dose-dependent manner. KNK437 also blocks the acquisition of thermotolerance that developed by sodium arsenite. [1]

KNK437 exerts low toxicity in vivo. In C3H/He mice transplanted with SCC VII cells, the concentration of KNK437 in the tumors gradually increases and reaches a peak 6 hours after i.p. injection. Hsp72 were synthesized 8 h after hyperthermia at 44 oC for 10 minutes, and their synthesis is inhibited by administration of KNK437 6 hours before hyperthermia. [2]

References:

1.  Yokota S, Kitahara M, Nagata K. Benzylidene lactam compound, KNK437, a novel

inhibitor of acquisition of thermotolerance and heat shock protein induction in

human colon carcinoma cells.  Cancer Res. 2000 Jun 1;60(11):2942-8.

2.  Koishi M, Yokota S, Mae T et al. The effects of KNK437, a novel inhibitor of heat shock protein

synthesis, on the acquisition of thermotolerance in a murine transplantable tumor in vivo.  Clin Cancer Res. 2001 Jan;7(1):215-9.