900515-16-4

Usage

Uses

Used in Pharmaceutical Industry:
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione is used as a PI3Kγ inhibitor for the development of therapeutic agents targeting inflammatory and immune disorders. Its selective inhibition of PI3Kγ makes it a promising candidate for treating conditions such as asthma, chronic obstructive pulmonary disease (COPD), and rheumatoid arthritis.
Used in Cancer Research:
In the field of cancer research, 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione is used as a potential anticancer agent. Its inhibitory effects on Casein kinase and PI3K p110α may contribute to the development of novel cancer therapies by targeting specific signaling pathways involved in tumor growth and progression.
Used in Drug Discovery:
5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione serves as a valuable compound in drug discovery efforts. Its unique chemical structure and inhibitory properties make it a useful tool for identifying new drug targets and developing innovative therapeutic agents for various diseases.
Used in Chemical Synthesis:
In the field of chemical synthesis, 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione can be used as a starting material or intermediate for the synthesis of other bioactive compounds. Its versatile structure allows for further modification and functionalization, enabling the development of new molecules with potential applications in various industries.

Biological Activity

as-252424 is a potent, selective and novel small-molecule pi3kγ inhibitor (ic50= 30 nm)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in thp-1 (human monocytic cell line), as-252424 inhibited the phosphorylation of pkb/akt due to mcp1 binding to the gpcr receptor ccr2 at lowest ic50 values of 0.4 μm. in primary monocytes and monocytic wild-type cell line thp-1, as-252424 inhibited mcp-1-mediated chemotaxis in a concentration-dependent manner (ic50 value= 52 μm and 53 μm, respectively). [1] in capan 1 and hpaf (pancreatic cancer cell lines), as52424 specifically inhibited the cell proliferation. [2]in a mouse model of thioglycollate-induced peritonitis, oral administration of as-252424 at 10 mg/kg led to moderate reduction of neutrophil recruitment (35% ±14%). [1]

Biochem/physiol Actions

AS-252424 is a potent and selective phosphoinositide 3-kinase PI3Kγ inhibitor with IC50 = 30 nM in a mouse model.

references

1. pomel v, klicic j, covini d et al. furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. j med chem. 2006 jun 29;49(13):3857-71.2. edling ce, selvaggi f, buus r et al. key role of phosphoinositide 3-kinase class ib in pancreatic cancer. clin cancer res. 2010 oct 15;16(20):4928-37.

Upstream product

• 900515-33-5 5-(4-fluoro-2-hydroxyphenyl)furan-2-carbaldehyde 
• 2295-31-0 thiazoline-2,4-dione 
• 147460-41-1 2-bromo-5-fluorophenol 
• 27329-70-0 5-formylfurane-2-boronic acid 
• 900515-32-4 5-(2-benzyloxy-4-fluorophenyl)furan-2-carbaldehyde 
• 202857-88-3 2-Benzyloxy-1-bromo-4-fluoro-benzene 

Relevant academic research and scientific papers

Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ

Class I phosphoinositide 3-kinases (PI3Ks), in particular PI3Kγ, have become attractive drug targets for inflammatory and autoimmune diseases. Here, we disclose a novel series of furan-2-ylmethylene thiazolidinediones as selective, ATP-competitive PI3Kγ i