CM 11

Cat. No. 6416 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： Homo-PROTAC^® for self-degradation of pVHL30

化学名： N¹,N²⁰-bis((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,6,9,12,15,18-hexaoxaicosanediamide

纯度： ≥98% (HPLC)

说明书

引用文献

文献 (2)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for CM 11

CM 11 is a PROTAC^® for self-degradation of the long form of VHL, pVHL30 (DC₅₀ < 100 nM). Composed of two VHL ligands joined by a linker. Exhibits > 1000-fold increased cellular activity compared to the parent VHL ligand, VH 032. Dimerizes pVHL30 with high avidity in vitro. Induced potent and rapid self-degradation of VHL in cell lines in a highly isoform dependent fashion. Negative control CMP 98 (Cat. No. 6417) also available.

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 CM 11

E3 ligase	VHL
DC₅₀	10-100 nM - Degradation of pVHL30 in HeLa cells after 24 h treatment
Selectivity confirmed by global proteomics	No
分子量	1179.46
公式	C₅₈H₈₂N₈O₁₄S₂
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	2244684-49-7
PubChem ID	134160242
InChI Key	WGJCHHJGGFCCRS-DEYDLUNASA-N
Smiles	CC1=C(C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=O)=O)=O)C=C2)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 CM 11

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	117.95	100

制备储备液 for CM 11

以下数据基于产品分子量 1179.46。 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.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	0.85 mL	4.24 mL	8.48 mL
5 mM	0.17 mL	0.85 mL	1.7 mL
10 mM	0.08 mL	0.42 mL	0.85 mL
50 mM	0.02 mL	0.08 mL	0.17 mL

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产品说明书 for CM 11

分析证书/产品说明书

化学品安全技术说明书

参考文献 for CM 11

参考文献是支持产品生物活性的出版物。

Maniaci et al (2017) Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat.Commun. 8 830 PMID: 29018234

If you know of a relevant reference for CM 11, please let us know.

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关键词: CM 11, CM 11 supplier, CM11, PROTACs, Proteolysis, targeted, chimeras, E3, ubiquitin, ligase, VHL, PROTAC, active, degraders, degrades, protein, degradation, tpd, Ubiquitin, Ligases, Ligase, Degraders, 6416, Tocris Bioscience

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TPD and Induced Proximity Research Product GuideUpdated

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

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