Potent inhibitor of mammalian HDACs (histone deacetylases) (IC50=15.7nM). Acts as a ligand for the enzyme active site metal ion. 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. Induces apoptosis in P-glyoprotein (Pgp) positive and Pgp negative multidrug resistant cells.
Product Details
| Alternative Name: | (2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic acid |
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| Formula: | C17H14N2O4S |
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| MW: | 342.4 |
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| CAS: | 151720-43-3 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | Tan to yellow solid. |
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| Solubility: | Soluble in DMSO, methanol or acetonitrile. |
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| Shipping: | Blue Ice |
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| Long Term Storage: | +4°C |
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| Handling: | Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Inhibitors of histone deacetylases: correlation between isoform specificity and reactivation of HIV type 1 (HIV-1) from latently infected cells: K. Huber, et al.; J. Biol. Chem.
286, 22211 (2011),
Abstract;
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Novel mechanisms of apoptosis induced by histone deacetylase inhibitors: M.J. Peart, et al.; Cancer Res.
63, 4460 (2003),
Abstract;
The novel anti-tumour agent oxamflatin differentially regulates urokinase and plasminogen activator inhibitor type 2 expression and inhibits urokinase-mediated proteolytic activity: A.E. Dear & R.L. Medcalf; Biochim. Biophys. Acta
1492, 15 (2000),
Abstract;
Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase: Y.B. Kim, et al.; Oncogene
18, 2461 (1999),
Abstract;
Oxamflatin: a novel compound which reverses malignant phenotype to normal one via induction of JunD: H. Sonoda, et al.; Oncogene
13, 143 (1996),
Abstract;
