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THAL SNS 032

Cat. No. 6532 2 篇引用文献 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 Cdk9 Degrader (PROTAC®)
化学名： N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献 (2)
评论
文献 (2)
生物活性 Scientific Data 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for THAL SNS 032

THAL SNS 032 is a degrader (PROTAC®) comprising the cyclin-dependent kinase inhibitor SNS 032 (Cat. No. 4075) conjugated to the cereblon E3 ligase ligand, thalidomide (Cat. No. 0652). Potent, selective and cereblon-dependent degrader of Cdk9 (EC50 = 4 nM). Displays >15-fold selectivity for Cdk9 over other CDKs (EC50 values are 62, 171 and 398 nM for Cdk2, Cdk1 and Cdk7, respectively). Induces complete degradation of Cdk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.

Cdk9 antibodies validated for Western Blot also available: Catalog # NBP2-15848 and NBP3-15345.

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

Scientific Data

Western Blot Application of THAL SNS 032 in MOLT-4 cells View Larger

Application of THAL SNS 032 in MOLT-4 cells. Western Blot data showing knockdown of both CDK9 isoforms after THAL SNS 032 treatment of MOLT-4 cells (4 h incubation). Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. Cdk9 primary antibody is used at 1:1000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems.Data courtesy of Jeff Cooper, Bio-Techne.

许可信息

Sold under license from Dana-Farber Cancer Institute.

技术数据 for THAL SNS 032

分子量 869.02
公式 C40H52N8O10S2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2139287-33-3
PubChem ID 131801483
InChI Key BXDZOYLPNAIDOC-UHFFFAOYSA-N
Smiles CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)CC(NCCOCCOCCOCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)C

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 THAL SNS 032

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 86.9 100

制备储备液 for THAL SNS 032

以下数据基于产品分子量 869.02。 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 1.15 mL 5.75 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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产品说明书 for THAL SNS 032

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for THAL SNS 032

参考文献是支持产品生物活性的出版物。

Olson et al (2018) Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat.Chem.Biol. 14 163 PMID: 29251720

If you know of a relevant reference for THAL SNS 032, please let us know.

按标靶查看相关产品

关键词: THAL SNS 032, THAL SNS 032 supplier, THALSNS032, potent, selective, CDK9, active, degraders, degrades, PROTAC, PROTACs, proteolysis, targeting, chimera, targeted, protein, degradation, tpd, Transcriptional, CDKs, Cyclin, Dependent, Kinase, (CDK), Degraders, 6532, Tocris Bioscience

2 篇 THAL SNS 032 的引用文献

引用文献是使用了 Tocris 产品的出版物。 THAL SNS 032 的部分引用包括：

Vladimir et al (2020) CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells. Cell Death Dis 11 754 PMID: 32934219

Kaji et al (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells Sci Rep 10 3088 PMID: 32080280

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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