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Submit ReviewMS 159 is a nuclear receptor binding SET structural domain protein 2 (NSD2) Degrader (DC50 = 5.2 μM, Dmax = >82%). Also degrades IKZF3 and IKZF1. Comprises an NSD2 binding moiety joined by a linker to a cereblon E3 ligase ligand. Inhibits proliferation of KMS11 and H929 tumor cells. Bioavailable in vivo.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
分子量 | 828.84 |
公式 | C43H40N8O10 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 3031353-59-7 |
PubChem ID | 164887575 |
InChI Key | OBZWKPGPTCBYOS-UHFFFAOYSA-N |
Smiles | O=C(NC1=NC=C(OCCCNC(CNC2=CC=CC3=C2C(N(C4CCC(NC4=O)=O)C3=O)=O)=O)C=C1)C(C=C5)=CC=C5CN(C(C6=CC7=C(NC(CO7)=O)C=C6)=O)C8CC8 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 41.44 | 50 |
以下数据基于产品分子量 828.84。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 2.41 mL | 12.07 mL | 24.13 mL |
2.5 mM | 0.48 mL | 2.41 mL | 4.83 mL |
5 mM | 0.24 mL | 1.21 mL | 2.41 mL |
25 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Meng et al (2022) Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos. J.Med.Chem. 65 10611 PMID: 35895319
If you know of a relevant reference for MS 159, please let us know.
关键词: MS 159, MS 159 supplier, MS159, degrader, degrades, degradation, NSD2, nuclear, receptor, binding, SET, structural, domain, protein, 2, PROTAC, proteolysis, targeting, chimeras, CRBN, cereblon, E3, ligase, WHSC1, MMSET, Other, Degraders, 8079, Tocris Bioscience
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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。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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