SNIPER(ER)-87

Modify Date: 2024-01-09 09:44:36

SNIPER(ER)-87 Structure
SNIPER(ER)-87 structure
Common Name SNIPER(ER)-87
CAS Number 2222354-91-6 Molecular Weight 1044.30
Density N/A Boiling Point N/A
Molecular Formula C59H73N5O10S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name SNIPER(ER)-87

 SNIPER(ER)-87 Biological Activity

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].
Related Catalog
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].
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.

[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.

 Chemical & Physical Properties

Molecular Formula C59H73N5O10S
Molecular Weight 1044.30