You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!Submit Review
α1A-AR Degrader 9c New
Biological Activity for α1A-AR Degrader 9c
α1A-AR Degrader 9c is a selective α1A-adrenergic receptor Degrader (PROTAC®; DC50 = 2.86 µM, 94% α1A-adrenoceptor degradation at 10 µM for 12 h). It comprises the α-adrenoceptor antagonist Prazosin (Cat. No. 0623), joined by a linker to a cereblon ligand Pomalidomide (Cat. No. 6302). α1A-AR Degrader 9c selectively downregulates α1A-adrenoceptor levels, but not α1B-AR and α1D-AR in HEK293 cells. α1A-AR Degrader 9c shows concentration-dependent antiproliferative activity in PC-3 prostate cancer cells (IC50 = 6.12 µM) in vitro, and PC-3 tumor xenografts in vivo.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for α1A-AR Degrader 9c
|Storage||Store at -20°C|
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 α1A-AR Degrader 9c
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for α1A-AR Degrader 9c
The following data is based on the product molecular weight 829.83. 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||1.21 mL||6.03 mL||12.05 mL|
|5 mM||0.24 mL||1.21 mL||2.41 mL|
|10 mM||0.12 mL||0.6 mL||1.21 mL|
|50 mM||0.02 mL||0.12 mL||0.24 mL|
Product Datasheets for α1A-AR Degrader 9c
References for α1A-AR Degrader 9c
References are publications that support the biological activity of the product.
Li et al (2020) First small-molecule PROTACs for G protein-coupled receptors: inducing α1A-adrenergic receptor degradation. Acta.Pharm.Sin.B 10 1669 PMID: 33088687
If you know of a relevant reference for α1A-AR Degrader 9c, please let us know.
View Related Products by Target
Keywords: a1A-AR Degrader 9c, a1A-AR Degrader 9c supplier, Selective, α1A, alpha, 1A, a1A, adrenergic, receptor, adrenoceptor, Degraders, degrades, targeted, protein, degradation, TPD, Active, Adrenergic, Alpha-1, Receptors, 7278, Tocris Bioscience
Citations for α1A-AR Degrader 9c
Citations are publications that use Tocris products.
Currently there are no citations for α1A-AR Degrader 9c. Do you know of a great paper that uses α1A-AR Degrader 9c from Tocris? Please let us know.
Reviews for α1A-AR Degrader 9c
There are currently no reviews for this product. Be the first to review α1A-AR Degrader 9c and earn rewards!
Have you used α1A-AR Degrader 9c?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Custom Degrader Services
- Ubiquitin-Proteasome System Proteins and Assays
- Assays for Protein Degradation
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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