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JH-XI-10-02

Cat. No. 7304 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： CDK8 Degrader (PROTAC®)
化学名： 15-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-N-[(3β,5α,17β)-17-(7-isoquinolinyl)androstan-3-yl]-N-methyl-4,7,10,13-tetraoxapentadecanamide
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 JH-XI-10-02

JH-XI-10-02 is a CDK8 Degrader (PROTAC®) comprising the cereblon binding ligand Pomalidomide (Cat. No. 6302) joined by a linker to a CDK8 inhibitor. JH-XI-10-02 (1 μM) induces significant proteasome-dependent degradation of CDK8 in Jurkat cells after 24 h, with no significant effect on CDK19 levels.

CDK8 antibody validated for Western Blot also available: Catalog # NBP2-92972.

许可信息

Sold under license from Dana-Farber Cancer Institute.

技术数据 for JH-XI-10-02

分子量 920.16
公式 C53H69N5O9
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2209085-22-1
PubChem ID 145708490
InChI Key JECHBTRAPARMGI-GFTKVEOVSA-N
Smiles [H][C@@]12CC[C@@H]([C@]1(CC[C@]3([C@]2(CC[C@]4(C[C@@H](N(C(CCOCCOCCOCCOCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)C)CC[C@]34C)[H])[H])[H])C)C8=CC9=C(C=C8)C=CN=C9

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 JH-XI-10-02

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.01 50

制备储备液 for JH-XI-10-02

以下数据基于产品分子量 920.16。 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 2.17 mL 10.87 mL 21.74 mL
2.5 mM 0.43 mL 2.17 mL 4.35 mL
5 mM 0.22 mL 1.09 mL 2.17 mL
25 mM 0.04 mL 0.22 mL 0.43 mL

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

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参考文献 for JH-XI-10-02

参考文献是支持产品生物活性的出版物。

Hatcher et al (2018) Development of highly potent and selective steroidal inhibitors and degraders of CDK8. ACS Med.Chem.Lett. 9 540 PMID: 29937979

If you know of a relevant reference for JH-XI-10-02, please let us know.

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关键词: JH-XI-10-02, JH-XI-10-02 supplier, CDK8, degraders, protacs, cyclin-dependent, kinases, targeted, protein, degradation, TPD, degrades, Transcriptional, CDKs, Cyclin, Dependent, Kinase, (CDK), Degraders, 7304, 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
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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