218924-25-5 Usage
Uses
Used in Pharmaceutical Industry:
3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM is used as a pharmaceutical compound for its potential therapeutic effects. It may be utilized in the development of new drugs targeting specific diseases or conditions, due to its ability to interact with various biological molecules and pathways.
Used in Research Applications:
In the field of research, 3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM serves as a valuable tool for studying the mechanisms of various biological processes. It can be used to investigate the effects of the compound on cell viability, apoptosis, and other cellular functions, contributing to a better understanding of its potential applications in medicine.
Used in Heat Shock Protein Inhibition:
3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM, also known as KNK437, is used as a heat shock factor 1 (HSF1) inhibitor and a heat shock protein 70 (HSP70) inhibitor. It has been studied for its effects on the inhibition of viability and apoptosis activation in chemoresistant mice cells, as well as its impact on the viability and apoptosis of colorectal cancer cells. Additionally, it has been shown to suppress morphine analgesic tolerance in rodent models, suggesting its potential use in pain management and addiction research.
Used in Inflammatory Response Modulation:
KNK437 has been studied for its effects on glutamine-induced HSP70 and inflammatory mediator release. This suggests that 3,4-METHYLENEDIOXY-BENZYLIDINE-GAMMA-BUTYROLACTAM may have potential applications in modulating the inflammatory response, which could be beneficial in the treatment of various inflammatory diseases and conditions.
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
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
Check Digit Verification of cas no
The CAS Registry Mumber 218924-25-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,8,9,2 and 4 respectively; the second part has 2 digits, 2 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 218924-25:
(8*2)+(7*1)+(6*8)+(5*9)+(4*2)+(3*4)+(2*2)+(1*5)=145
145 % 10 = 5
So 218924-25-5 is a valid CAS Registry Number.
