IDR E804 Dark red solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 µM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin. Purity: ≥95% by HPLC. Ref.: Nam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998. |
