SNIPER(ER)-87

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SNIPER(ER)-87 

SNIPER(ER)-87 由凋亡蛋白 (IAP) 配体 LCL161 衍生物的抑制剂组成，该抑制剂通过 PEG 接头与雌激素受体 α (ERα) 配体 4-Hydroxytamoxifen 缀合，并有效降解 ERα 蛋白 (IC50=0.097 μM)。SNIPER(ER)-87 在细胞中优先招募 XIAP 至 ERα，而 XIAP 是负责 SNIPER(ER)-87 诱导的 ERα 降解的主要 E3 泛素连接酶。

SNIPER(ER)-87

SNIPER(ER)-87 Chemical Structure

CAS No. : 2222354-91-6

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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1044.30

Formula

C59H73N5O10S
CAS 号

2222354-91-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

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