dBET1

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Cat.No. 6327 - dBET1 | C38H37ClN8O7S | CAS No. 1799711-21-9
Description: (+)-JQ1 based PROTAC that selectively degrades BET bromodomains in cells
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

PROTAC comprising BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BET bromodomains in cancer cell lines in vitro (EC50 = 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 785.27
Formula C38H37ClN8O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1799711-21-9
PubChem ID 91799313
InChI Key LKEGXJXRNBALBV-PMCHYTPCSA-N
Smiles CC1=NN=C2[C@@H](N=C(C3=CC=C(C=C3)Cl)C4=C(N12)SC(C)=C4C)CC(NCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 78.53 100

Preparing Stock Solutions

The following data is based on the product molecular weight 785.27. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.27 mL 6.37 mL 12.73 mL
5 mM 0.25 mL 1.27 mL 2.55 mL
10 mM 0.13 mL 0.64 mL 1.27 mL
50 mM 0.03 mL 0.13 mL 0.25 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Winter et al (2015) Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370

Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579


If you know of a relevant reference for dBET1, please let us know.

Keywords: dBET1, supplier, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, degradation, Ubiquitin, E3, Ligases, PROTACs, Bromodomains, Ubiquitin, E3, Ligases, Tocris Bioscience

Citations for dBET1

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