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JPS016

Cat. No. 8083 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： Selective class I HDAC Degrader (PROTAC®)
化学名： (2S,4R)-1-((S)-2-(2-((9-(2-((4-((2-Aminophenyl)carbamoyl)phenyl)amino)-2-oxoethoxy)nonyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
纯度： ≥97% (HPLC)
说明书
引用文献
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文献 (3)
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 JPS016

JSP016 is a selective Degrader (PROTAC®) and inhibitor of class I HDACs (DC50 values are 530 nM and 550 nM for HDAC3 and HDAC1; Dmax is 77%, 66% and 45% at HDAC1, 3 and 2; IC50 values are 380 nM, 570 nM and 820 nM at HDAC3, 1 and 2). Comprises a benzamide-based compound joined by a linker to a Von Hippel Lindau (VHL) E3 ligase ligand. JPS016 treatment up- or down-regulates nearly 4000 differentially expressed genes, arrests cells at sub-G1 phase and promotes apoptosis in HCT116 cells.

许可信息

Sold under license from the University of Leicester

技术数据 for JPS016

分子量 898.13
公式 C48H63N7O8S
储存 Store at -20°C
纯度 ≥97% (HPLC)
CAS Number 2669785-77-5
PubChem ID 163322304
InChI Key BOXZMOCGSKLDAH-OUZJXKGJSA-N
Smiles NC(C=CC=C1)=C1NC(C(C=C2)=CC=C2NC(COCCCCCCCCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)=O)=O)=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 JPS016

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 8.98 10

制备储备液 for JPS016

以下数据基于产品分子量 898.13。 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
0.1 mM 11.13 mL 55.67 mL 111.34 mL
0.5 mM 2.23 mL 11.13 mL 22.27 mL
1 mM 1.11 mL 5.57 mL 11.13 mL
5 mM 0.22 mL 1.11 mL 2.23 mL

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参考文献 for JPS016

参考文献是支持产品生物活性的出版物。

Smalley et al (2022) Optimization of class I hstone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells. J.Med.Chem. 65 5642 PMID: 35293758

If you know of a relevant reference for JPS016, please let us know.

按标靶查看相关产品

关键词: JPS016, JPS016 supplier, PROTAC, proteolysis, targeting, chimera, chimeras, PROTACs, degrader, degraders, histone, deacetylase, HDAC, HDAC1, HDAC2, HDAC3, vhl, von, hippel, lindau, E3, ligase, Histone, Deacetylase, (HDAC), Degraders, Class, I, HDACs, 8083, 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!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

Epigenetics in Cancer Research Product Guide

Epigenetics in Cancer Research Product Guide

This product guide reviews some of the main areas in cancer epigenetics research and lists around 120 products that can be used for the main epigenetic targets including:

  • Histone Methylation
  • Histone Acetylation
  • DNA Methylation
  • Ubiquitination
  • Bromodomains
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
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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