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Description: TRIM24 degrading PROTAC
Chemical Name: (2S,4R)-1-((S)-15-(tert-Butyl)-1-(3-(N-(1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)sulfamoyl)phenyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity
PROTAC® composed of the TRIM24 ligand IACS-9571 conjugated to a VHL ligand. Displays dose- and time-dependent degradation of TRIM24 in cells, with maximum degradation achieved at 5 μM. Degradation phenotypically mirrors genetic deletion of TRIM24. Demonstrates antiproliferative effects in MOLM-13 cells. Cell permeable.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from Dana-Farber Cancer Institute
Technical Data
| M. Wt | 1113.3 |
| Formula | C55H68N8O13S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2170695-14-2 |
| PubChem ID | 131954388 |
| InChI Key | QUQTXFIMYFMULC-OGOZKGDESA-N |
| Smiles | CCCOC1=CC=CC(OC2=C(C=C3N(C(N(C3=C2)C)=O)C)NS(=O)(C4=CC(C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)=CC=C4)=O)=C1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.27 | 20 | |
| ethanol | 22.27 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 1113.3. 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 |
|---|---|---|---|
| 0.2 mM | 4.49 mL | 22.46 mL | 44.91 mL |
| 1 mM | 0.9 mL | 4.49 mL | 8.98 mL |
| 2 mM | 0.45 mL | 2.25 mL | 4.49 mL |
| 10 mM | 0.09 mL | 0.45 mL | 0.9 mL |
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References
References are publications that support the biological activity of the product.
Gechijian et al (2018) Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat.Chem.Biol. 14 405 PMID: 29507391
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Keywords: dTRIM 24, dTRIM 24 supplier, dTRIM24, degraders, degrades, PROTAC, proteolysis, targeting, chimera, PROTACs, TRIM24, Tripartite, motif-containing, 24, transcriptional, intermediary, factor, 1alpha, TIF1α, Active, Degraders, Other, Transcription, Factors, 6607, Tocris Bioscience
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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.
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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