SP 141

Description

Mouse double minute 2 protein (MDM2) is an E3 ubiquitin-protein ligase that binds and ubiquitinates the tumor suppressor p53, leading to its degradation by the proteasome. SP 141 is a cell-permeable inhibitor of MDM2 (K_i = 28 nM). Binding of MDM2 by SP 141 promotes its auto-ubiquitination and proteasomal degradation. SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo. This compound has a short half-life in plasma and wide tissue distribution in tumor-bearing nude mice.

The Uses of SP 141

SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines, inhibiting xenograft tumor growth in vivo.

Storage

Store at +4°C

References

[1]. vassilev lt, vu bt, graves b, et al. in vivo activation of the p53 pathway by small-molecule antagonists of mdm2. science. 2004 feb 6;303(5659):844-8.
[2]. wang w, qin jj, voruganti s, et al. the pyrido[b]indole mdm2 inhibitor sp-141 exerts potent therapeutic effects in breast cancer models. nat commun. 2014 oct 1;5:5086.
[3]. wang w, qin jj, voruganti s, et al. identification of a new class of mdm2 inhibitor that inhibits growth of orthotopic pancreatic tumors in mice. gastroenterology. 2014 oct;147(4):893-902.e2.
[4]. nag s, qin jj, voruganti s, et al. development and validation of a rapid hplc method for quantitation of sp-141, a novel pyrido[b]indole anticancer agent, and an initial pharmacokinetic study in mice. biomed chromatogr. 2015 may;29(5):654-63.