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Biological Activity for CG 858
CG 858 is a selective BRAF-V600E protein Degrader (uSMITETM). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide (Cat. No. 0652). CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). Exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.
CG 858 negative control (Cat. No. 7428) also available.
Sold under license from Cullgen.
Technical Data for CG 858
|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 CG 858
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for CG 858
The following data is based on the product molecular weight 839.87. 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||1.19 mL||5.95 mL||11.91 mL|
|5 mM||0.24 mL||1.19 mL||2.38 mL|
|10 mM||0.12 mL||0.6 mL||1.19 mL|
|50 mM||0.02 mL||0.12 mL||0.24 mL|
References for CG 858
References are publications that support the biological activity of the product.
Han et al (2020) Discovery of selective small molecule degraders of BRAF-V600E. J.Med.Chem. 63 4069 PMID: 32223235
If you know of a relevant reference for CG 858, please let us know.
View Related Products by Target
Keywords: CG 858, CG 858 supplier, CG858, degraders, targeted, protein, degradation, degrades, E3, ligase, uSMITE, BRAF-V600E, kinase, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, PROTAC, Active, Degraders, Raf, Kinase, 7427, Tocris Bioscience
Citations for CG 858
Citations are publications that use Tocris products.
Currently there are no citations for CG 858. Do you know of a great paper that uses CG 858 from Tocris? Please let us know.
Reviews for CG 858
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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 GuideUpdated
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
- Ubiquitin-Proteasome System Proteins
- 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
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