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HHP 9

Cat. No. 7828 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： BET bromodomain Degrader (PROTAC®); also potent Hedgehog pathway inhibitor
化学名： 2-Methoxyethyl 4-(3-((1-(6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-7-(2-methoxyphenyl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
纯度： ≥98% (HPLC)
说明书
引用文献
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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 HHP 9

HHP 9 is a potent BET bromodomain Degrader (PROTAC®; DC50 values are 0.03 μM, 0.2 μM and 0.2 μM at BRD3, BRD2 and BRD4 respectively). BRD2, BRD3 and BRD4 are almost completely degraded by HHP 9 in vitro (after 27h incubation with 0.5 - 5 μM of HHP 9). Comprises a Hedgehog Pathway Inhibitor-1 (HPI-1, Cat. No. 3839) coupled to a CRBN ligand. BET bromodomain degradation through HPP-9 results in long-acting Hh pathway inhibition.

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

技术数据 for HHP 9

分子量 900.99
公式 C49H52N6O11
储存 Store at -20°C
纯度 ≥98% (HPLC)
InChI Key RJNFQVDPIFXYAO-UHFFFAOYSA-N
Smiles CC1=C(C(OCCOC)=O)C(C2=CC(OCC3=CN(CCCCCCOC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)N=N3)=CC=C2)C7=C(N1)CC(C8=C(OC)C=CC=C8)CC7=O

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 HHP 9

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 90.1 100

制备储备液 for HHP 9

以下数据基于产品分子量 900.99。 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 1.11 mL 5.55 mL 11.1 mL
5 mM 0.22 mL 1.11 mL 2.22 mL
10 mM 0.11 mL 0.55 mL 1.11 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

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参考文献 for HHP 9

参考文献是支持产品生物活性的出版物。

Bagka et al (2023) Targeted protein degradation reveals BET bromodomains as the cellular target of Hedgehog pathway inhibitor-1. Nat.Commun. 14 3893 PMID: 37393376

If you know of a relevant reference for HHP 9, please let us know.

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关键词: HHP 9, HHP 9 supplier, HHP9, PROTACs, Degraders, degrades, potent, BET, bromodomains, BRD2, BRD3, BRD4, HPI-1, Hedgehog, Pathway, Inhibitor-1, CRBN, Signaling, Bromodomains, Bromodomain, (BRD), 7828, Tocris Bioscience

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该领域的文献

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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:

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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