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dBET6

Cat. No. 6945 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 (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
化学名： (6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
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 dBET6

dBET6 is a potent and selective Degrader (PROTAC®) of BET bromodomains (IC50 = ~10 nM). dBET6 comprises BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines through BRD4 degradation. Induces apoptosis. Reduces leukemic burden in a mouse model of T-ALL. Cell permeable.

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

许可信息

Sold under license from Dana-Farber Cancer Institute

技术数据 for dBET6

E3 ligase CRBN
DC50 / Dmax 6 nM / 97% - Degradation of BRD4 in HEK293T cells after 3 h treatment
Kd (Degrader to Target) 46 nM - Kd of BRD4 BD1 was assessed by FP
Selectivity confirmed by global proteomics Yes
分子量 841.38
公式 C42H45ClN8O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1950634-92-0
PubChem ID 121427831
InChI Key JGQPZPLJOBHHBK-UFXYQILXSA-N
Smiles CC1=NN=C2[C@H](CC(=O)NCCCCCCCCNC(=O)COC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1

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 dBET6

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 84.14 100

制备储备液 for dBET6

以下数据基于产品分子量 841.38。 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 1.19 mL 5.94 mL 11.89 mL
5 mM 0.24 mL 1.19 mL 2.38 mL
10 mM 0.12 mL 0.59 mL 1.19 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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参考文献 for dBET6

参考文献是支持产品生物活性的出版物。

Winter et al (2017) BET Bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol. Cell 67 5 PMID: 28673542

Verstovsek et al (2017) Targeting cistrome and dysregulated transcriptome of post-MPN sAML. Oncotarget 8 93301 PMID: 29212143

Nowak et al (2018) Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat.Chem.Biol. 14 706 PMID: 29892083

If you know of a relevant reference for dBET6, please let us know.

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关键词: dBET6, dBET6 supplier, Potent, selective, active, degraders, degrades, BET, bromodomains, BRD4, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, degradation, JQ1, cell, permeable, in, vivo, tpd, Bromodomains, Bromodomain, (BRD), Degraders, 6945, Tocris Bioscience

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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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