AG-490

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AG-490_structure.png



AG-490 is a chemical compound known for its role as an inhibitor of the Janus kinase (JAK) family of enzymes. It is primarily used in research settings to study the JAK/STAT signaling pathway, which is critical in various cellular processes including growth, survival, and differentiation.

Mechanism of Action[edit | edit source]

AG-490 functions by inhibiting the activity of Janus kinases, particularly JAK2. This inhibition prevents the phosphorylation and activation of Signal Transducer and Activator of Transcription (STAT) proteins, thereby blocking the downstream signaling pathways that lead to gene expression. The JAK/STAT pathway is involved in the signaling of various cytokines and growth factors, making AG-490 a valuable tool in studying diseases where this pathway is dysregulated, such as certain cancers and inflammatory conditions.

Applications in Research[edit | edit source]

AG-490 has been extensively used in preclinical studies to investigate its effects on cancer cell lines. It has shown potential in inhibiting the growth of leukemia, breast cancer, and prostate cancer cells by inducing apoptosis and cell cycle arrest. Additionally, AG-490 has been used to study the role of JAK/STAT signaling in immune responses and inflammatory diseases.

Pharmacokinetics[edit | edit source]

While AG-490 is primarily used in vitro, studies have explored its pharmacokinetic properties in animal models. It is known to have a relatively short half-life and limited bioavailability, which has restricted its use in clinical settings. However, its effectiveness in modulating JAK/STAT signaling continues to make it a compound of interest in drug development research.

Safety and Toxicity[edit | edit source]

As with many research chemicals, the safety profile of AG-490 is not fully established for human use. In laboratory settings, it is handled with care to avoid exposure, and its effects are studied under controlled conditions. Researchers are advised to follow standard safety protocols when working with AG-490.

Also see[edit | edit source]

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Contributors: Prab R. Tumpati, MD