CRBN PROTAC® 14a

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说明: Cereblon Degrader (PROTAC®)
化学名: N1-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-N20-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,9,12,18-tetraoxaicosanediamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)

生物活性 for CRBN PROTAC® 14a

CRBN PROTAC® 14a is a cereblon Degrader (PROTAC®). Comprises a ligand for Von Hippel Lindau (VHL) protein joined by a linker to a cereblon targeting ligand. Preferentially degrades cereblon (DC50 = 200 nM in HEK293 cells). Induces rapid and profound cereblon degradation (98% decrease after 8 h at 1 μM in HEK293 cells).

CRBN antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # NBP1-91810.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

许可信息

Sold under licence from the University of Dundee

技术数据 for CRBN PROTAC® 14a

分子量 1061.26
公式 C53H72N8O13S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2358775-70-7
PubChem ID 138911387
InChI Key PEZCAXDTKNFUCR-CTMFSBKBSA-N
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCCCCOCCOCCCCCOCC(NCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)=O)O)=O)SC=N1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CRBN PROTAC® 14a

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 106.13 100

制备储备液 for CRBN PROTAC® 14a

以下数据基于产品分子量 1061.26。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 0.94 mL 4.71 mL 9.42 mL
5 mM 0.19 mL 0.94 mL 1.88 mL
10 mM 0.09 mL 0.47 mL 0.94 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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产品说明书 for CRBN PROTAC® 14a

参考文献 for CRBN PROTAC® 14a

参考文献是支持产品生物活性的出版物。

Girardini et al (2019) Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg.Med.Chem. 27 2466 PMID: 30826187


If you know of a relevant reference for CRBN PROTAC® 14a, please let us know.

关键词: CRBN PROTAC® 14a, CRBN PROTAC® 14a supplier, PROTACs, PROTAC, proteolysis, targeting, chimera, active, Degrader, Degraders, degrading, VHL, von, Hippel, Lindau, Cereblon, CRBN, targeted, protein, degradation, TPD, Ubiquitin, E3, Ligases, Ligase, 7219, Tocris Bioscience

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该领域的文献

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia