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说明： PRC1 Degrader (PROTAC®); degrades BMI1 and RING1B
化学名： (2S,4R)-1-((S)-2-(7-(5-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)phenyl)piperazin-1-yl)pentanamido)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride
纯度： ≥97% (HPLC)
生物活性 for MS 147
MS 147 is a polycomb repressive complex 1 (PRC1) Degrader (PROTAC®) (Kd values are 450 nM and 3 μM for VHL and EED, respectively). Comprises an EED binder (EED 226, Cat. No. 7762) joined by a linker to a VHL E3 ligase ligand. MS 147 preferentially degrades BMI1 and RING1B and reduces H2AK119ub in K562 cells. Inhibits proliferation in cancer cell lines that are insensitive to EZH2 knockout or EED/PRC2 Degraders.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
许可信息
Sold under license from Icahn School of Medicine at Mount Sinai.
Important Information for MS 147
This product is sold as an HCl salt. The stoichiometry of the salt and hydration levels vary from batch to batch. It is sold in gross weight and the batch specific Molecular Weight is available on the Certificate of Analysis.
技术数据 for MS 147
| M. Wt | 1015.29 (Free Base) |
| 公式 | C54H70N12O6S.xHCl |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| InChI Key | WZUKNVLQEQHTMY-RTJWYONCSA-N |
| Smiles | CC1=C(C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCCCCNC(CCCCN4CCN(C5=CC=C(C6=CN=C(NCC7=CC=CO7)N8C6=NN=C8)C=C5)CC4)=O)=O)C(C)(C)C)=O)=O)C=C2)SC=N1.Cl |
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 MS 147
| 溶解性 | Soluble to 50 mg/ml in DMSO |
产品说明书 for MS 147
参考文献 for MS 147
参考文献是支持产品生物活性的出版物。
Park et al (2023) Targeted degradation of PRC1 components, BMI1 and RING1B, via a novel protein complex degrader strategy. Adv.Sci. (Weinh.) 10 e2205573 PMID: 36737841
If you know of a relevant reference for MS 147, please let us know.
关键词: MS 147, MS 147 supplier, MS147, PROTAC, PROTACS, degrader, degrades, degraders, VHL, von, hippel, lindau, proteolysis, targeting, chimera, PRC1, polycomb, repressive, complex, BMI1, RING1B, H2AK119ub, Polycomb, Repressive, Complex, (PRC), Degraders, 8077, 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。
TPD and Induced Proximity Research Product GuideUpdated
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
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