A cell-permeable tripyrrole alkaloid compound that displays immunosuppressive and anti-tumor properties irrespective of p53 status and multidrug resistance. Shown to selectively upregulate p21WAF/CIP1 and NAG-1 (nonsteroidal anti-inflammatory drug-activated gene 1) and downregulate survivin expression levels, induce mitochondria-mediated apoptosis and cell cycle arrest in tumor cells. Prevents FADD phosphorylation (IC50=2.0uM in A549-FKR cells) through inhibition of FADD-kinase CK1a (IC50 ~6.0uM in SW620-BGCR cells) and augments cisplatin -induced apoptosis. Blocks NF-kB activation by decreasing plkBa (by 63% at 3uM) and lkBa levels in A549 cells, and shrinks tumor growth in A549-FKR tumor xenograft mouse model (3mg/kg, i.p., o.d.).
Formula:C20H25N3O
Molecular Weight:323.4
Solubility:DMSO, DMF, EtOH, MeOH
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
