所有图片(3)
别名:
1-氧-4-氨基-2-（2,6-二氧哌啶-3-基）异吲哚, 3-（4-氨基-1,3-二氢-1-氧代-2H-异吲哚-2-基）-2,6-哌啶二酮, 3-（4-氨基-1-氧代异吲哚-2-基）哌啶-2,6-二酮, E3连接酶配体, 用于PROTAC® >研究的配体
经验公式（希尔记法）:
C13H13N3O3
推荐产品
ligand
lenalidomide
检测方案
≥95%
形式
powder
反应适用性
reagent type: ligand
mp
265-268 °C
储存温度
2-8°C
SMILES字符串
O=C1N(C2CCC(NC2=O)=O)CC3=C1C=CC=C3N
InChI
1S/C13H13N3O3/c14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18/h1-3,10H,4-6,14H2,(H,15,17,18)
InChI key
GOTYRUGSSMKFNF-UHFFFAOYSA-N
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应用
来那度胺被证明是一种可与Cereblon（CRBN）蛋白结合的配体。来那度胺和其他沙利度胺衍生物可用于构建用于靶向蛋白质降解和 PROTAC（靶向蛋白降解嵌合体）技术的小分子。 探索 蛋白质降解剂合成砌块，E3连接酶配体-Linker结合物简化了PROTAC的合成和文库生成。
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其他说明
法律信息
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
相关产品
产品编号
说明
价格
警示用语：
Danger
危险声明
危险分类
Repr. 1B - STOT RE 2
靶器官
Blood
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Inchul You et al.
Cell chemical biology, 27(1), 66-73 (2019-12-21)
The PI3K/AKT signaling cascade is one of the most commonly dysregulated pathways in cancer, with over half of tumors exhibiting aberrant AKT activation. Although potent small-molecule AKT inhibitors have entered clinical trials, robust and durable therapeutic responses have not been
Jan Krönke et al.
Science (New York, N.Y.), 343(6168), 301-305 (2013-12-03)
Lenalidomide is a drug with clinical efficacy in multiple myeloma and other B cell neoplasms, but its mechanism of action is unknown. Using quantitative proteomics, we found that lenalidomide causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1
Richard J Visconti et al.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 36(10), 1914-1930 (2021-06-27)
Human myeloma bone disease (MBD) occurs when malignant plasma cells migrate to the bone marrow and commence inimical interactions with stromal cells, disrupting the skeletal remodeling process. The myeloma cells simultaneously suppress osteoblastic bone formation while promoting excessive osteoclastic resorption.
Guangyan Du et al.
Cell chemical biology, 29(10), 1470-1481 (2022-09-08)
Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major bottleneck in the TPD field is the lack of accessible E3 ligase ligands for developing degraders.
Gang Lu et al.
Science (New York, N.Y.), 343(6168), 305-309 (2013-12-03)
Thalidomide-like drugs such as lenalidomide are clinically important treatments for multiple myeloma and show promise for other B cell malignancies. The biochemical mechanisms underlying their antitumor activity are unknown. Thalidomide was recently shown to bind to, and inhibit, the cereblon
商品
Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
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