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Description: HECT E3 ubiquitin ligase inhibitor
Chemical Name: N-(4-Acetylphenyl)-3-(5-ethyl-2-furanyl)-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity for Heclin
Heclin 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.
Compound Libraries for Heclin
Heclin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Heclin
| M. Wt | 283.32 |
| Formula | C17H17NO3 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Heclin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.33 | 100 | |
| ethanol | 14.17 | 50 |
Preparing Stock Solutions for Heclin
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for Heclin
References for Heclin
References are publications that support the biological activity of the product.
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.
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Keywords: Heclin, Heclin supplier, E6-AP, carboxyl, terminus, HECT, E3, ubiquitin, ubiquitination, inhibitors, inhibits, inhibts, NAMs, negative, allosteric, modulators, Ubiquitin, Ligases, 5433, Tocris Bioscience
4 Citations for Heclin
Citations are publications that use Tocris products. Selected citations for Heclin include:
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
Do you know of a great paper that uses Heclin from Tocris? Please let us know.
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Literature in this Area
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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
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- Assays for Protein Degradation
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Programmed Cell Death Poster
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.
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