Organosulfur Compounds
AdipoGen TPEN
Chemical. CAS 16858-02-9. Formula C26H28N6. MW 424.5. TPEN is a cell permeable metal ion chelator. TPEN is a chelator that has a high affinity for zinc Zn2, next to other transition metals Zn2 >Fe2 >Mn2 and is used in zinc treatment studies to limit intra- and extracellular concentrations of the mineral. TPEN has lower affinity for Ca2 and Mg2 and can also form complexes with other soft metal ions such as Cd2. In addition to a heavy metal chelator, TPEN is also known to be an apoptosis inducer. Depletion of zinc by TPEN induces apoptosis in several cell lines. TPEN shows anticancer activity through induction of caspase-dependent apoptosis, via reactive oxygen species ROS signaling mechanism and inhibiting cell autophagy. TPEN also inhibits RNA binding protein Lin28 and has been shown to be useful in extracting Abeta depostis from Alzheimers disease brain tissue.
AdipoGen TPEN
Chemical. CAS 16858-02-9. Formula C26H28N6. MW 424.5. TPEN is a cell permeable metal ion chelator. TPEN is a chelator that has a high affinity for zinc Zn2, next to other transition metals Zn2 >Fe2 >Mn2 and is used in zinc treatment studies to limit intra- and extracellular concentrations of the mineral. TPEN has lower affinity for Ca2 and Mg2 and can also form complexes with other soft metal ions such as Cd2. In addition to a heavy metal chelator, TPEN is also known to be an apoptosis inducer. Depletion of zinc by TPEN induces apoptosis in several cell lines. TPEN shows anticancer activity through induction of caspase-dependent apoptosis, via reactive oxygen species ROS signaling mechanism and inhibiting cell autophagy. TPEN also inhibits RNA binding protein Lin28 and has been shown to be useful in extracting Abeta depostis from Alzheimers disease brain tissue.
AdipoGen PTACH
Chemical. CAS 848354-66-5. Formula C20H26N2O2S2. MW 390.56. Synthetic. Non-hydroxamate HDAC inhibitor HDACi IC50 32, 48 and 41nM for HDAC4, HDAC1 and HDAC6, respectively. Cell-permeable prodrug that is intracellularly converted to a potent HDAC inhibitor. Predicted to exhibit a similar HDAC binding mode as that of SAHA, interacting with the active-site zinc targeting group. Shown to exhibit comparable antiproliferative and apoptotic activity as SAHA against various cancer cell lines. Inhibits growth of various cancer cells in vitro EC50 = 1.1 - 9.1mM. Also reactivates latent HIV-1 gene expression.
AdipoGen PTACH
Chemical. CAS 848354-66-5. Formula C20H26N2O2S2. MW 390.56. Synthetic. Non-hydroxamate HDAC inhibitor HDACi IC50 32, 48 and 41nM for HDAC4, HDAC1 and HDAC6, respectively. Cell-permeable prodrug that is intracellularly converted to a potent HDAC inhibitor. Predicted to exhibit a similar HDAC binding mode as that of SAHA, interacting with the active-site zinc targeting group. Shown to exhibit comparable antiproliferative and apoptotic activity as SAHA against various cancer cell lines. Inhibits growth of various cancer cells in vitro EC50 = 1.1 - 9.1mM. Also reactivates latent HIV-1 gene expression.