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AT6

Catalog No.GC33354

AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).

Products are for research use only. Not for human use. We do not sell to patients.

AT6 Chemical Structure

Cas No.: 2098836-50-9

Size Price Stock Qty
1mg
$270.00
In stock
5mg
$585.00
In stock
10mg
$945.00
In stock
25mg
$1,935.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AT6 is a PROTAC AT1 analogue, which is a highly selective bromodomain (Brd4) degrader.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that recruit a target protein in proximity to an E3 ubiquitin ligase to trigger protein degradation. Structural elucidation of the key ternary ligase: PROTAC: target species and how this impacts target degradation selectivity remains elusive. The ligand folds into itself to allow formation of specific intermolecular interactions in the ternary complex. Isothermal titration calorimetry studies, supported by surface mutagenesis and proximity assays, are consistent with pronounced cooperative formation of ternary complexes with Brd4BD2. Structure-based-designed compound AT1 exhibits highly selective depletion of Brd4 in cells[1].

[1]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.

Chemical Properties

Cas No. 2098836-50-9 SDF
Canonical SMILES CC1=C(C)C(C(C2=CC=C(Cl)C=C2)=N[C@@H](CC(NCCOCCOCCSC(C)(C)[C@H](NC(C)=O)C(N3C[C@H](O)C[C@H]3C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)=O)=O)C6=NN=C(C)N67)=C7S1
Formula C48H58ClN9O7S3 M.Wt 1004.68
Solubility Soluble in DMSO Storage Store at -20°C, protect from light, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.9953 mL 4.9767 mL 9.9534 mL
5 mM 0.1991 mL 0.9953 mL 1.9907 mL
10 mM 0.0995 mL 0.4977 mL 0.9953 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 7 reference(s) in Google Scholar.)

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