AT 1

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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)
Citations (3)
Reviews (1)
Literature (4)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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.

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, Protein, Degraders, Bromodomains, (BRD), 6356, Tocris Bioscience

3 Citations for AT 1

Citations are publications that use Tocris products. Selected citations for AT 1 include:

Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation. J Am Chem Soc 145 1593 PMID: 36626587

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

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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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.

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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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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.

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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

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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