AT 1
Tocris Bioscience, part of Bio-Techne | Catalog # 6356
(+)-JQ1 based PROTAC® with selectivity for BRD4
Key Product Details
Description
(+)-JQ1 based PROTAC® with selectivity for BRD4
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 DundeeProduct Specifications
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for AT 1
For research use only
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