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LL-K9-3

Cat. No. 7813 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 HyT-based degrader of the CDK9-cyclin T1 complex
化学名： N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-1-[[2-[[2-[[(1R,2S,5R)-5-methyl-2-(1-methylethyl)cyclohexyl]oxy]acetyl]amino]ethyl]sulfonyl]-4-piperidinecarboxamide
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 LL-K9-3

LL-K9-3 is a selective hydrophobic tagging technologies (HyT)-based Degrader of the CDK9-cyclin T1 complex (DC50 values are 589 and 662 nM for cyclin T1 and CDK9, respectively). It comprises a CDK9 inhibitor, SNS 032 (Cat. No. 4075), joined by a glycol linker to hydrophobic tag. LL-K9-3 exhibits no degradation of other CDKs (CDK1, 2, 4, 5, 6, and 7). In 22RV1 cells. LL-K9-3 reduces expression of androgen receptor (AR) and cMyc by inducing selective and synchronous degradation of CDK9 and cyclin T1.

技术数据 for LL-K9-3

分子量 683.94
公式 C31H49N5O6S3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2809353-52-2
PubChem ID 164946948
InChI Key NPRIWHDFWDSJRZ-YFNKSVMNSA-N
Smiles O=S(CCNC(CO[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)=O)(N2CCC(CC2)C(NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3)=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 LL-K9-3

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 68.39 100
ethanol 3.42 5

制备储备液 for LL-K9-3

以下数据基于产品分子量 683.94。 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 1.46 mL 7.31 mL 14.62 mL
5 mM 0.29 mL 1.46 mL 2.92 mL
10 mM 0.15 mL 0.73 mL 1.46 mL
50 mM 0.03 mL 0.15 mL 0.29 mL

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参考文献 for LL-K9-3

参考文献是支持产品生物活性的出版物。

Li et al (2022) Discovery of small-molecule degraders of the CDK9-cyclin T1 complex for targeting transcriptional addiction in prostate cancer. J.Med.Chem. 65 11034 PMID: 35925880

If you know of a relevant reference for LL-K9-3, please let us know.

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关键词: LL-K9-3, LL-K9-3 supplier, LL-K9-3, PROTAC, degraders, degrades, hydrophobic, tagging, technologies, HyT, SNS, 032, CDK9-cyclin, T1, complex, prostate, cancer, Transcriptional, CDKs, Cyclin, Dependent, Kinase, (CDK), Degraders, 7813, 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