SNIPER(ER)-87 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1044.30

C₅₉H₇₃N₅O₁₀S

2222354-91-6

Solid

White to off-white

C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=CC(OCCOCCOCCOCC(N(C)CCOC5=CC=C(/C(C6=CC=C(O)C=C6)=C(C7=CC=CC=C7)\CC)C=C5)=O)=C4)=O)=CS3)CCC2)=O)=O

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• [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.  [Content Brief]

  [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.  [Content Brief]