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Radicicol inhibits p60<SUP>v-<I>src</I></SUP> kinase activity, and tyrosine phosphorylation of p53/56<I><SUP>lyn</I>.<SUP>1,</SUP><SUP>2</SUP> </P> <P>The specific inhibition of the chaperone Hsp90 confers anticancer properties to Radicicol.<SUP>3,</SUP><SUP>4</SUP> In eukaryotic cells, Hsp90 catalyzes the final activation step of many regulatory proteins. Cells that lose Hsp90 function are severely compromised and cannot progress through the cell cycle.</P> <P>Radicicol, similarly to Geldanamycin, binds to the nucleotide-binding pocket, and inhibits ATPase activity of Hsp90.<SUP>5</SUP> This causes destabilization of Hsp90 client proteins (v-Src, Raf-1, ErbB2 Ras), many of which are essential for tumor cell growth.<SUP>6</SUP> Oncogene induced transformation of NIH 3T3 cells (src, ras, and mos) is suppressed by radicicol and it also disrupts the K-Ras-activated signaling pathways by selective depletion of Raf kinase.<SUP>7,</SUP><SUP>8</SUP> In addition, it also exhibits anti-angiogenic activity <I>in vivo</I>, and reduces the expression of VEGF.<SUP>9,</SUP><SUP>10</SUP> </P> <P>Radicicol inhibits AP-1-, NF-<FONT face=Symbol>k</FONT>B- and serum response factor (SRF)-mediated transcription.<SUP>11</SUP> It inhibits the expression of COX-2 without affecting COX-1 expression in LPS-stimulated macrophages,<SUP>1</SUP> and induces the differentiation of HL-60 cells into macrophages, by blocking the cell cycle at G1 and G2 sites.<SUP>12</P> </FONT></font><br/> <table><tr><td><B><FONT color="#527592" face="arial" size="2">M.W.:</FONT></B></td><td><font face="arial" size="2">364.8</font></td></tr></table><br/><table><tr><td><B><FONT color="#527592" face="arial" size="2">CAS No.:</FONT></B></td><td><font face="arial" size="2"><FONT size=2> <P>[12772-57-5]</P></FONT></font></td></tr></table><br/><table><tr><td><B><FONT color="#527592" face="arial" size="2">Structure:</FONT></B></td></tr><tr><td><font face="arial" size="2"><FONT color=#ffffff>.</FONT></font></td></tr></table><table><tr><td><img src="http://www.alomone.com/p_postcards/database/R-370.gif"/></td> <td valign="bottom"><font face="arial" size="2"></font></td></tr></table><br/><table><tr><td><B><FONT color="#527592" face="arial" size="2">Purity:</FONT></B></td><td><font face="arial" size="2">>99% </font></td></tr></table><br/><table><tr><td><B><FONT color="#527592" face="arial" size="2">Bioassay:</FONT></B></td></tr><tr><td><font face="arial" size="2"><FONT size=2> <P>The biological activity was tested to confirm the ability of Radiciol to inhibit cell proliferation.</P></FONT></font></td></tr></table><table><tr><td><img src="http://www.alomone.com/p_postcards/database/R-370b.gif"/></td> </tr><tr><td valign="bottom"><font face="arial" size="2">Hela (blue), WEHI (pink) or Jurkat (red) cells were grown in presence of different concentrations of Radicicol for 4 days. <BR>Then the cell quantity was measured using the XTT or Methylene blue method. <BR>The cell quantity versus Radicicol concentrations is presented in the figure.</font></td></tr></table><table></table> <p><a href="http://penitrem.4mg.com/">penitrem</a> | <a href="http://puromycin.4mg.com">puromycin</a> | <a href="http://radicicol.4mg.com/">radicicol</a> | <a href="http://rapamycin.4mg.com/">rapamycin</a> | <a href="http://sterigmatocystin.4mg.com/">sterigmatocystin</a> | 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