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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)
Literature (4)

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.

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
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.

Solubility Data for BRD PHOTAC-I-3

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.77 50

Preparing Stock Solutions for BRD PHOTAC-I-3

The following data is based on the product molecular weight 935.45. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.14 mL 10.69 mL 21.38 mL
2.5 mM 0.43 mL 2.14 mL 4.28 mL
5 mM 0.21 mL 1.07 mL 2.14 mL
25 mM 0.04 mL 0.21 mL 0.43 mL

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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

If you know of a relevant reference for BRD PHOTAC-I-3, please let us know.

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, Active, Bromodomains, 7319, Tocris Bioscience

Citations for BRD PHOTAC-I-3

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

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
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  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
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Epigenetics Scientific Review

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

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

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