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Submit ReviewHeclin is a HECT E3 ubiquitin ligase inhibitor; inhibits Nedd4, Smurf2 and WWP1 (IC50 values are 6.3, 6.8 and 6.9 μM respectively). Selective for HECT-mediated over RING-mediated ubiquitination.
Heclin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 283.32 |
公式 | C17H17NO3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 890605-54-6 |
PubChem ID | 7464118 |
InChI Key | SPTWXRJNCFIDRQ-ZHACJKMWSA-N |
Smiles | CC(C1=CC=C(NC(/C=C/C2=CC=C(CC)O2)=O)C=C1)=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 | 28.33 | 100 | |
ethanol | 14.17 | 50 |
以下数据基于产品分子量 283.32。 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 | 3.53 mL | 17.65 mL | 35.3 mL |
5 mM | 0.71 mL | 3.53 mL | 7.06 mL |
10 mM | 0.35 mL | 1.76 mL | 3.53 mL |
50 mM | 0.07 mL | 0.35 mL | 0.71 mL |
参考文献是支持产品生物活性的出版物。
Mund et al (2014) Peptide and small molecule inhibitors of HECT-type ubiquitin ligases. Proc.Natl.Acad.Sci.U.S.A. 111 16736 PMID: 25385595
If you know of a relevant reference for Heclin, please let us know.
关键词: Heclin, Heclin supplier, E6-AP, carboxyl, terminus, HECT, E3, ubiquitin, ubiquitination, inhibitors, inhibits, inhibts, NAMs, negative, allosteric, modulators, Ubiquitin, Ligases, 5433, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Heclin 的部分引用包括:
Yang et al (2020) Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysise Biochem Pharmacol 180 PMID: 32592721
Cheng-Wei et al (2022) Tyrphostin AG1024 Suppresses Coronaviral Replication by Downregulating JAK1 via an IR/IGF-1R Independent Proteolysis Mediated by Ndfip1/2_NEDD4-like E3 Ligase Itch. Pharmaceuticals (Basel) 15 PMID: 35215353
Yingxian et al (2020) The E3 ubiquitin ligase Smurf2 regulates PARP1 stability to alleviate oxidative stress-induced injury in human umbilical vein endothelial cells. J Cell Mol Med 24 4600-4611 PMID: 32167680
Saskia C et al (2020) Myocardial infarction affects Cx43 content of extracellular vesicles secreted by cardiomyocytes. Life Sci Alliance 3 PMID: 33097557
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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