958852-01-2 Usage
Description
5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione, also known as GSK 1059615, is a potent inhibitor of PI 3-kinase α (PI3Kα) and FRAP (mTOR). It is a small molecule compound with a complex chemical structure that has been developed for its potential therapeutic applications.
Uses
Used in Cancer Therapy:
GSK 1059615 is used as an anticancer agent, particularly for inhibiting the proliferation of cancer cells. It targets the PI3K/AKT/mTOR signaling pathway, which plays a crucial role in cell growth, survival, and metabolism. By inhibiting PI3Kα and mTOR, GSK 1059615 can attenuate MAPK signaling and reduce the growth and survival of cancer cells.
Used in Drug Development:
GSK 1059615 is used as a research tool in drug development for the identification and optimization of novel PI3K and mTOR inhibitors. Its potent inhibitory activity against these targets makes it a valuable compound for studying the role of the PI3K/AKT/mTOR pathway in various diseases, including cancer.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, GSK 1059615 is used as a lead compound for the development of new drugs targeting the PI3K/AKT/mTOR pathway. Its unique chemical structure and inhibitory properties provide a foundation for the design and synthesis of more potent and selective inhibitors for therapeutic applications.
Used in Academic Research:
GSK 1059615 is used in academic research to study the molecular mechanisms underlying the regulation of the PI3K/AKT/mTOR pathway and its role in various cellular processes, such as cell growth, survival, and metabolism. This research can provide valuable insights into the development of new therapeutic strategies for the treatment of cancer and other diseases associated with dysregulation of this pathway.
Biological Activity
gsk1059615 is inhibitor of pan-pi3k with ic50 values of 0.4nm, 0.6nm, 5nm, 2nm and 12nm for pi3kα, p13kβ, p13kγ, p13kδ and mtor, respectively [1].gsk1059615 is a potent and reversible inhibitor of p13k. it also has inhibition efficacy to the oncogenic mutants of pi3kα. the thiazolidinedione ring of gsk1059615 forms an interaction with the catalytic lysine (lys833) within the atp-binding pocket. in cellular assay, gsk1059615 is reported to induce g1 arrest and apoptosis in a variety of cell lines. among these, the breast tumor cells display more sensitive. moreover, gsk1059615 significantly suppresses tumor growth and increases plasma insulin levels in xenograft mice [1, 2].
references
[1] carnero a. novel inhibitors of the pi3k family. 2009.[2] knight s d, adams n d, burgess j l, et al. discovery of gsk2126458, a highly potent inhibitor of pi3k and the mammalian target of rapamycin. acs medicinal chemistry letters, 2010, 1(1): 39-43.
Check Digit Verification of cas no
The CAS Registry Mumber 958852-01-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,5,8,8,5 and 2 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 958852-01:
(8*9)+(7*5)+(6*8)+(5*8)+(4*5)+(3*2)+(2*0)+(1*1)=222
222 % 10 = 2
So 958852-01-2 is a valid CAS Registry Number.
958852-01-2Relevant articles and documents
THIAZOLIDINEDIONE DERIVATIVES AS PI3 KINASE INHIBITORS
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, (2008/06/13)
Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.
