Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewAT 1
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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
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.
View Related Products by Target
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, Active, Degraders, Bromodomains, 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.)
Have you used AT 1?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Filter by:
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
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.
Targeted Protein Degradation Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Ubiquitin-Proteasome System Proteins
- Assays for Protein Degradation
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
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