dBET1

Name: dBET1
Brand: Tocris Bioscience
SKU: 6327

Tocris Bioscience, part of Bio-Techne | Catalog # 6327

Citations (2)

COA / SDS

(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo

Key Product Details

Description:	(+)-JQ1 based Degrader (PROTAC^®) targeting BET bromodomains, active in vivo
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)
Molecular Weight:	785.27

View Full Technical Details for dBET1

Technical Data
Citations

Biological Activity for dBET1

dBET1 is a Degrader (PROTAC^®) comprising BET bromodomain 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. Antibody validated for Western Blot also available: NBP2-77359.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data for dBET1

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for dBET1

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

Preparing Stock Solutions for dBET1

The following data is based on the product molecular weight 785.27.

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	1.27 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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References for dBET1

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

Wurz A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 2017 PMID: 28378579
Winter Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 2015 PMID: 25999370