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Submit ReviewJPS036 is a selective HDAC3 Degrader (PROTAC®) (DC50 = 440 nM; Dmax = 77 %). JPS036 comprises a benzamide-based compound joined by a linker to a Von Hippel Lindau (VHL) E3 ligase ligand.
Negative control JPS016NC also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from the University of Leicester
分子量 | 940.19 |
公式 | C51H66FN7O7S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2669785-85-5 |
PubChem ID | 156808378 |
InChI Key | NAADBQUVFJWCFU-XVYMMXEDSA-N |
Smiles | O=C(C1(CC1)F)N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=C(C=C(C4=C(N=CS4)C)C=C3)OCCCCCCCCCCCC(NC5=CC=C(C=C5)C(NC6=C(C=CC=C6)N)=O)=O)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 18.8 | 20 温和加热 |
以下数据基于产品分子量 940.19。 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 |
---|---|---|---|
0.2 mM | 5.32 mL | 26.59 mL | 53.18 mL |
1 mM | 1.06 mL | 5.32 mL | 10.64 mL |
2 mM | 0.53 mL | 2.66 mL | 5.32 mL |
10 mM | 0.11 mL | 0.53 mL | 1.06 mL |
参考文献是支持产品生物活性的出版物。
Smalley et al (2022) Optimization of class I histone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells. J.Med.Chem. 65 5642 PMID: 35293758
If you know of a relevant reference for JPS036, please let us know.
关键词: JPS036, JPS036 supplier, JPS036, HDAC3, protac, degrader, degraders, degrades, selective, VHL, von, hippel, lindau, Protein, Degraders, PROTACs, proteolysis, targeting, chimera, active, Class, I, HDACs, Histone, Deacetylase, (HDAC), 8085, 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