SNIPER(ER)-87 consists of an inhibitor ofapoptosisprotein (IAP) ligand LCL161 derivative that is conjugated to theestrogen receptorα (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades theERαprotein (IC₅₀=0.097 μM). SNIPER(ER)-87 preferentially recruitsXIAPtoERαin the cells, andXIAPis the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-inducedERαdegradation^[1][2].

SNIPER(ER)-87 (0.1-1000 nM; 72 hours) efficiently inhibits the ERα-dependent transcriptional activation by β-estradiol and suppresses the growth of ERα-positive breast tumor cells with IC₅₀s of 15.6 nM in MCF-7 and 9.6 nM in T47D cells^[1].

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].

1044.30

C₅₉H₇₃N₅O₁₀S

2222354-91-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.