(2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic Acid Solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable, aromatic sulfonamide derivative with a hydroxamic acid group that potently inhibits mammalian histone deacetylase (IC50 = 15.7 nM) by binding to the active site Zinc. Augmented the expression of transcription factor JunD and causes an inhibition of transformation in K-ras-transformed NIH3T3 cells (MIC ~40 nM). Upregulates plasminogen activator inhibitor type 2 (PAI-2) expression with concomitant inhibition of urokinase (u-PA) gene and protein expression in HT-1080 and U-937 cells. Elevates the expression of extracellular matrix proteins fibronectin and gelsolin. Purity: ≥95% by HPLC. Ref.: Lavoie, R., et al. 2001. Bioorg. Med. Chem. Lett. 11, 2847. Dear, A.E., and Medcalf, R.L. 2000. Biochim. Biophys. Acta. 1492, 15. Kim, Y.B., et al. 1999. Oncogene 18, 2461. Ohtani, M., et al. 1996. J. Med. Chem. 39, 2871. Sonoda, H., et al. 1996. Oncogene 13, 143. |
