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Submit ReviewBRD PHOTAC-I-3
Description: Photoswitchable BET bromodomain Degrader (PHOTAC)
Chemical Name: 2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f]-[1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(4-((E)-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)diazenyl)-2,6-dimethoxyphenoxy)acetamido)butyl)acetamide
Purity: ≥98% (HPLC)
Biological Activity for BRD PHOTAC-I-3
BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1 (Cat. No. 4499). Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark. BRD2 antibodies validated for Western Blot also available: Catalog # NBP1-30475 and NBP2-75422.
Licensing Information
Sold under license from New York University
Technical Data for BRD PHOTAC-I-3
| M. Wt | 935.45 |
| Formula | C46H47ClN10O8S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2370997-94-5 |
| PubChem ID | 154722038 |
| InChI Key | SGZZPSOQAWRZGE-RCBZUBGNSA-N |
| Smiles | COC1=CC(/N=N/C2=C3CN(C(C3=CC=C2)=O)C4CCC(NC4=O)=O)=CC(OC)=C1OCC(NCCCCNC(C[C@@H]5N=C(C6=CC=C(C=C6)Cl)C7=C(N8C(C)=NN=C58)SC(C)=C7C)=O)=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.
Product Datasheets for BRD PHOTAC-I-3
References for BRD PHOTAC-I-3
References are publications that support the biological activity of the product.
Reynders et al (2020) PHOTACs enable optical control of protein degradation. Sci.Adv. 6 eaay5064 PMID: 32128406
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Keywords: BRD PHOTAC-I-3, BRD PHOTAC-I-3 supplier, PHOTAC, PHOtochemically, TArgeting, Chimeras, chimaeras, photoswitch, photoswitchable, light, activated, BET, bromodomains, BRD2, BRD3, BRD4, Degraders, degrades, targeted, protein, degradation, Bromodomains, Bromodomain, (BRD), 7319, Tocris Bioscience
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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
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
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