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CG 428 is a potent tropomyosin receptor kinase (TRK) Degrader (uSMITETM) (DC50 = 0.36 nM). CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide (Cat. No. 6302). CG 428 shows selectivity for TRKA over TRKC and TRKB (Kd values = 1nM, 4.2 nM and 28 nM, respectively). Inhibits growth of KM12 colon cancer cells (IC50 =2.9 nM) and is bioavailable.
Negative control also available, CG 428-Neg (Cat. No. 7426).
Sold under license from Cullgen
|DC50||0.36 nM (TMP3-TRKA), 2.23 nM (TRKA) - Degradation in KM12/HEL cells after 6 h treatment|
|Kd (Degrader to Target)||1 nM - Kd was assessed using the KINOMEscan assay|
|IC50 (Cellular Activity)||2.9 nM - Inhibits growth of KM12 cells|
|Selectivity confirmed by global proteomics||No|
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 814.88. 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||1.23 mL||6.14 mL||12.27 mL|
|5 mM||0.25 mL||1.23 mL||2.45 mL|
|10 mM||0.12 mL||0.61 mL||1.23 mL|
|50 mM||0.02 mL||0.12 mL||0.25 mL|
References are publications that support the biological activity of the product.
Chen et al (2020) Discovery of first-in-class potent and selective tropomyosin receptor kinase degraders. J.Med.Chem. 63 14562 PMID: 33058680
If you know of a relevant reference for CG 428, please let us know.
Keywords: CG 428, CG 428 supplier, CG428, degraders, uSMITE, E3, ligase, TRK, tropomyosin, receptors, kinases, potent, selective, PROTAC, targeted, protein, degradation, Ubiquitin-mediated, Small, Molecule-Induced, Target, Elimination, Active, Degraders, Other, Kinases, 7425, Tocris Bioscience
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
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.
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.
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