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SNIPER(ER)-87 

Cat. No.: HY-129619
Handling Instructions

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.

For research use only. We do not sell to patients.

SNIPER(ER)-87 Chemical Structure

SNIPER(ER)-87 Chemical Structure

CAS No. : 2222354-91-6

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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 (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 Vitro

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].

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].

Molecular Weight

1044.30

Formula

C₅₉H₇₃N₅O₁₀S

CAS No.

2222354-91-6

SMILES

C[[email protected]](NC)C(N[[email protected]@H](C1CCCCC1)C(N2[[email protected]](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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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SNIPER(ER)-87PROTACEstrogen Receptor/ERRProteolysis-targeting chimeraInhibitorinhibitorinhibit

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SNIPER(ER)-87
Cat. No.:
HY-129619
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