BRD PHOTAC-I-3

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说明: Photoswitchable BET bromodomain Degrader (PHOTAC)
化学名: 2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f]-[1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(4-((E)-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)diazenyl)-2,6-dimethoxyphenoxy)acetamido)butyl)acetamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)

生物活性 for BRD PHOTAC-I-3

BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1 (Cat. No. 4499). Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark. BRD2 antibodies validated for Western Blot also available: Catalog # NBP1-30475 and NBP2-75422.

许可信息

Sold under license from New York University

技术数据 for BRD PHOTAC-I-3

分子量 935.45
公式 C46H47ClN10O8S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2370997-94-5
PubChem ID 154722038
InChI Key SGZZPSOQAWRZGE-RCBZUBGNSA-N
Smiles COC1=CC(/N=N/C2=C3CN(C(C3=CC=C2)=O)C4CCC(NC4=O)=O)=CC(OC)=C1OCC(NCCCCNC(C[C@@H]5N=C(C6=CC=C(C=C6)Cl)C7=C(N8C(C)=NN=C58)SC(C)=C7C)=O)=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 BRD PHOTAC-I-3

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.77 50

制备储备液 for BRD PHOTAC-I-3

以下数据基于产品分子量 935.45。 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
0.5 mM 2.14 mL 10.69 mL 21.38 mL
2.5 mM 0.43 mL 2.14 mL 4.28 mL
5 mM 0.21 mL 1.07 mL 2.14 mL
25 mM 0.04 mL 0.21 mL 0.43 mL

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参考文献 for BRD PHOTAC-I-3

参考文献是支持产品生物活性的出版物。

Reynders et al (2020) PHOTACs enable optical control of protein degradation. Sci.Adv. 6 eaay5064 PMID: 32128406


If you know of a relevant reference for BRD PHOTAC-I-3, please let us know.

关键词: BRD PHOTAC-I-3, BRD PHOTAC-I-3 supplier, PHOTAC, PHOtochemically, TArgeting, Chimeras, chimaeras, photoswitch, photoswitchable, light, activated, BET, bromodomains, BRD2, BRD3, BRD4, Degraders, degrades, targeted, protein, degradation, Bromodomains, Bromodomain, (BRD), 7319, 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