STAT5 Inhibitor

Signal Transducers and Activators of Transcriptions (STATs) are a family of cytoplasmic latent transcription factors that are activated to regulate gene expression in response to a large number of extracellular signaling polypeptides including cytokines, interferons, and growth factors.^1,2,3 STAT5, which consists of two isoforms STAT5α and STAT5β, is known to be overactive in several kinds of leukemias and various solid tumors. STAT5 Inhibitor is a cell-permeable, nonpetidic nicotinoyl hydrazone that suppresses STAT5 by targeting its SH2 domain (IC₅₀ = 47 µM against STAT5β SH2 domain EPO peptide binding activity).⁴ Comparatively, this compound exhibits reduced potency towards inhibiting the SH2 domain of STAT1, STAT3, or Lck (IC₅₀ > 500 µM).⁴ STAT5 Inhibitor has been shown to block STAT5/STAT5 DNA binding in K562 nuclear extracts.⁴

WARNING This product is not for human or veterinary use.

1. Leonard, W.J., and O'Shea, J.J. Jaks and STATs: Biological implications. Annu. Rev. Immunol. 16, 293-322 (1998).

2. Schindler, C., and Darnell, J.E., Jr. Transcriptional responses to polypeptide ligands: The JAK-STAT pathway. Annu. Rev. Biochem. 64, 621-562 (2011).

3. Darnell, J.E., Jr. STATs and gene regulation. Science 277(5332), 1630-1635 (1997).

4. Müller, J., Sperl, B., Reindl, W., et al. Discovery of chromone-based inhibitors of the transcription factor STAT5. Chembiochem 9(5), 723-727 (2008).