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Submit ReviewPomalidomide is a potent TNF-α inhibitor (IC50 = 13 nM). Also potently inhibits IL-2 (EC50 = 8 nM). Thalidomide derivative. Binds cereblon and inhibits its ubiquitination. Exhibits antiproliferative effects in a Namalwa lymphoma cell line. Antiangiogenic. Promotes degradation of transcription factor SALL4.
分子量 | 273.24 |
公式 | C13H11N3O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 19171-19-8 |
PubChem ID | 134780 |
InChI Key | UVSMNLNDYGZFPF-UHFFFAOYSA-N |
Smiles | NC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=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 | 27.32 | 100 |
以下数据基于产品分子量 273.24。 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 |
---|---|---|---|
1 mM | 3.66 mL | 18.3 mL | 36.6 mL |
5 mM | 0.73 mL | 3.66 mL | 7.32 mL |
10 mM | 0.37 mL | 1.83 mL | 3.66 mL |
50 mM | 0.07 mL | 0.37 mL | 0.73 mL |
参考文献是支持产品生物活性的出版物。
Lohbeck & Miller (2016) Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development. Bioorg.Med.Chem.Lett. 26 5260 PMID: 27687673
Nanthakumar et al (2015) Dissecting fibrosis: therapeutic insights from the small-molecule toolbox. Nat.Rev.Drug.Discov. 14 693 PMID: 26338155
Lai et al (2016) Modular PROTAC design for the degradation of oncogenic BCR-ABL. Angew.Chem.Int.Ed.Engl. 55 807 PMID: 26593377
Winter et al (2015) Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 348 1376 PMID: 25999370
Donovan et al (2018) Thal. promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome. Elife 7 e38430 PMID: 30067223
Chamberlain et al (2019) Evolution of cereblon-mediated protein degradation as a therapeutic modality. ACS Med.Chem.Lett. 10 1592 PMID: 31857833
If you know of a relevant reference for Pomalidomide, please let us know.
关键词: Pomalidomide, Pomalidomide supplier, Pomalidomide, TNFa, TNFalpha, TNFα, Inhibitors, inhibits, IL-2, thalidomide, cereblon, binder, ubiquitination, antiproliferative, antiangiogenic, lymphoma, SALL4, CELMoD, E3, ligase, modulators, immunomodulators, immunomodulatory, imide, IMiDs, Ubiquitin, Ligases, Cytokines, Antiangiogenics, Other, Transcription, Factors, Molecular, Glues, 6302, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Pomalidomide 的部分引用包括:
Francisca et al (2022) Systematic profiling of conditional degron tag technologies for target validation studies. Nat Commun 13 5495 PMID: 36127368
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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:
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
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