| Chemical Properties | Back Directory | [Boiling point ]
1100.3±65.0 °C(Predicted) | [density ]
1.209±0.06 g/cm3(Predicted) | [solubility ]
Soluble to 100 mM in DMSO | [pka]
9.38±0.15(Predicted) |
| Hazard Information | Back Directory | [Description]
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein | [Uses]
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation[1][2]. | [in vivo]
SNIPER(ER)-87 (30 mg/kg, i.p., every 24 h for 14 days) inhibits the growth of MCF-7 orthotopic breast tumor xenografts in 6-week-old female BALB/c nude mice[1]. | [storage]
Store at -20°C | [References]
[1] Ohoka N, et al. In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs). J Biol Chem. 2017 Mar 17;292(11):4556-4570. DOI:10.1074/jbc.M116.768853
[2] Ohoka N, et al. Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation. J Biol Chem. 2018 May 4;293(18):6776-6790. DOI:10.1074/jbc.RA117.001091 |
|
|