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CRBN-6-5-5-VHL

Cat. No. 6948 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective cereblon Degrader (PROTAC®); cell-permeable
化学名： (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
纯度： ≥96% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 Scientific Data 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for CRBN-6-5-5-VHL

CRBN-6-5-5-VHL is a potent and selective cereblon Degrader (PROTAC®) (DC50 = 1.5 nM). Induces complete degradation of cereblon in MM1S cells. Comprises a cereblon E3 ligase ligand joined by a linker to a ligand for the E3 ligase VHL. Cell-permeable.

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.

Scientific Data

Western Blot Application of CRBN-6-5-5-VHL in MM1S cells for CRBN-6-5-5-VHL View Larger

Application of CRBN-6-5-5-VHL in MM1S cells for CRBN-6-5-5-VHL. Western blot data showing potent knockdown of Cereblon (CRBN) mediated by the Degrader: CRBN-6-5-5-VHL in MM1S cells after 16 h incubation. IKZF1 (Ikaros) and IKZF3 (Aiolos) are transcription factors and neosubstrates of Cereblon. Application of CRBN-6-5-5-VHL does not result in degradation of these proteins. Pom; Pomalidomide. Data courtesy of Christian Steinebach, University of Bonn.

技术数据 for CRBN-6-5-5-VHL

分子量 972.21
公式 C51H69N7O10S
储存 Store at -20°C
纯度 ≥96% (HPLC)
CAS Number 2362575-45-7
Smiles CC1=C(SC=N1)C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCCOCCCCCOCCCCCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)=O)C(C)(C)C)=O)=O)C=C2

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-6-5-5-VHL

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 97.22 100

制备储备液 for CRBN-6-5-5-VHL

以下数据基于产品分子量 972.21。 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 1.03 mL 5.14 mL 10.29 mL
5 mM 0.21 mL 1.03 mL 2.06 mL
10 mM 0.1 mL 0.51 mL 1.03 mL
50 mM 0.02 mL 0.1 mL 0.21 mL

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产品说明书 for CRBN-6-5-5-VHL

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参考文献 for CRBN-6-5-5-VHL

参考文献是支持产品生物活性的出版物。

Steinebach et al (2019) PROTAC-mediated crosstalk between E3 ligases. Chem.Commun.(Camb) 55 1821 PMID: 30672516

If you know of a relevant reference for CRBN-6-5-5-VHL, please let us know.

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关键词: CRBN-6-5-5-VHL, CRBN-6-5-5-VHL supplier, PROTACs, proteolysis, targeting, chimeras, active, Degraders, degrades, VHL, von, Hippel, Lindau, Cereblon, CRBN, PROTAC, targeted, protein, degradation, tpd, Ubiquitin, E3, Ligases, Ligase, 6948, 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