AT 1

Tocris Bioscience | Catalog # 6356

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

Key Product Details

Description

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

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

Product Specifications for AT 1

Molecular Weight

972.68

Formula

C48H58ClN9O5S3

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

Product Documents for AT 1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for AT 1

For research use only

Customer Reviews for AT 1 (1)

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  • AT1 PROTAC
    Name: Anonymous
    Species: Human
    Assay Type: In Vitro
    Cell Line/Tissue: glioblastoma
    Verified Customer | Posted 07/24/2020
    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.
    AT 1 6356

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