SIM1

Pricing Availability   Qty
说明: Potent and selective trivalent BET Bromodomain Degrader (PROTAC®)
化学名: N,N'-(11-((2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)

生物活性 for SIM1

SIM1 is a potent and selective trivalent PROTAC® Degrader based on BET bromodomain inhibitors linked to a Von Hippel Lindau (VHL) ligand via branched linkers. SIM1 degrades all BET family proteins with a preference for BRD2 (DC50 values = 0.7 nM, 1.1 nM and 3.3 nM for BRD4, BRD2 and BRD3, respectively). SIM1 degrades BRD2 more significantly and rapidly than BRD3 and BRD4, and degrades BET proteins with a higher potency than a bivalent degrader. SIM1 also decreases protein levels for Myc and HMOX1 and induces apoptosis in prostate cancer cells.

许可信息

Sold under licence from the University of Dundee

技术数据 for SIM1

分子量 1618.82
公式 C79H98Cl2N14O13S3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2719051-84-8
PubChem ID 156022820
InChI Key RARNTROXRCXFHV-CMRSQZKGSA-N
Smiles CC1=C(C)C2=C(S1)N1C(C)=NN=C1[C@H](CC(=O)NCCOCCOCCOCC(C)(COCCOCCOCCNC(=O)C[C@@H]1N=C(C3=C(SC(C)=C3C)N3C(C)=NN=C13)C1=CC=C(Cl)C=C1)COCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1=CC=C(C=C1)C1=C(C)N=CS1)C(C)(C)C)N=C2C1=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 SIM1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 80.94 50

制备储备液 for SIM1

以下数据基于产品分子量 1618.82。 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 1.24 mL 6.18 mL 12.35 mL
2.5 mM 0.25 mL 1.24 mL 2.47 mL
5 mM 0.12 mL 0.62 mL 1.24 mL
25 mM 0.02 mL 0.12 mL 0.25 mL

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参考文献 for SIM1

参考文献是支持产品生物活性的出版物。

Imaide et al (2021) Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity Nat.Chem.Biol. 17 1157 PMID: 34675414


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关键词: SIM1, SIM1 supplier, targeted, protein, degradation, degraders, trivalent, VHL, von, hippel, lindau, E3, ligases, bromodomains, PROTAC, BET, BRD2, Bromodomain, (BRD), Degraders, 7432, 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