AT 1

Name: AT 1
Brand: Tocris Bioscience
SKU: 6356
Rating: 5 (1 reviews)

Catalog # 6356 | Tocris Bioscience a Bio-Techne Brand

(1)

Citations (3)

COA / SDS

(+)-JQ1 based PROTAC® with selectivity for BRD4

Key Product Details

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)
Molecular Weight:	972.68

View Full Technical Details for AT 1

Technical Data
Citations (3) / Reviews (1)

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 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	0.10 mL	0.51 mL	1.03 mL
50 mM	0.02 mL	0.10 mL	0.21 mL

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References for AT 1

References are publications that support the biological activity of the product.

Gadd Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 2017 PMID: 28288108

Citations for AT 1 (3)

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Citations are publications that use Bio-Techne 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

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AT1 PROTAC

Name: Anonymous

Species: Human

Assay Type: In Vitro

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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