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Description: (+)-JQ1 based PROTAC® with selectivity for BRD4
Chemical Name: (2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyrrolidinine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for AT 1
AT 1 is a cell penetrant Proteolysis Targeting Chimera (PROTAC®) compound based on (+)-JQ1 (Cat. No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Rationally designed based on a ternary complex crystal structure to improve selectivity for BRD4 degradation compared to MZ1 (Cat. No. 6154). Demonstrates profound and selective degradation of BRD4 in cells at 1-3 μM, with negligible loss of BRD2 and BRD3.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license
Licensing Information
Sold under licence from the University of Dundee
Technical Data for AT 1
| M. Wt | 972.68 |
| Formula | C48H58ClN9O5S3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2098836-45-2 |
| PubChem ID | 124201841 |
| InChI Key | SQNZDYHMCMIGGV-TZPPCSJFSA-N |
| Smiles | CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCCCCCSC(C)(C)[C@H](NC(C)=O)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)C7=NN=C(C)N27 |
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 AT 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 97.27 | 100 | |
| ethanol | 97.27 | 100 |
Preparing Stock Solutions for AT 1
The following data is based on the product molecular weight 972.68. 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 | 1.03 mL | 5.14 mL | 10.28 mL |
| 5 mM | 0.21 mL | 1.03 mL | 2.06 mL |
| 10 mM | 0.1 mL | 0.51 mL | 1.03 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.21 mL |
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Product Datasheets for AT 1
References for AT 1
References are publications that support the biological activity of the product.
Gadd (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 13 514 PMID: 28288108
If you know of a relevant reference for AT 1, please let us know.
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Keywords: AT 1, AT 1 supplier, PROTAC, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, AT1, PROTACs, active, degraders, degrades, protein, degradation, tpd, Bromodomains, (BRD), Degraders, 6356, Tocris Bioscience
3 Citations for AT 1
Citations are publications that use Tocris products. Selected citations for AT 1 include:
Lin et al (2021) Time-dependent effect of 1,6-hexanediol on biomolecular condensates and 3D chromatin organization. Genome Biol 22 230 PMID: 34404453
Eric S et al (2021) Chemo-proteomics exploration of HDAC degradability by small molecule degraders. Cell Chem Biol 28 1514-1527.e4 PMID: 34314730
Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation. J Am Chem Soc 145 1593 PMID: 36626587
Do you know of a great paper that uses AT 1 from Tocris? Please let us know.
Reviews for AT 1
Average Rating: 5 (Based on 1 Review.)
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AT1 PROTAC.
By
Anonymous on 07/24/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: glioblastoma
We tested the effect of AT1 PROTAC in degrading the endogenous BRD4 protein in glioblastoma cell lines with varying concentrations of AT1 starting from 100nM, 300nM and 1 uM.
Literature in this Area
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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