dBET6

Name: dBET6
Brand: Tocris Bioscience
SKU: 6945

Tocris Bioscience, part of Bio-Techne | Catalog # 6945

Citations (3)

COA / SDS

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

Key Product Details

Description:	Potent and selective (+)-JQ1 based Degrader (PROTAC^®) targeting BET bromodomains, active in vivo
Chemical Name:	(6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-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:	841.38

View Full Technical Details for dBET6

Technical Data
Citations

Biological Activity for dBET6

dBET6 is a potent and selective Degrader (PROTAC^®) of BET bromodomains (IC₅₀ = ~10 nM). dBET6 comprises BET antagonist (+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines through BRD4 degradation. Induces apoptosis. Reduces leukemic burden in a mouse model of T-ALL. Cell permeable.

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 dBET6

M. Wt	841.38
Formula	C₄₂H₄₅ClN₈O₇S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1950634-92-0
PubChem ID	121427831
InChi Key	JGQPZPLJOBHHBK-UFXYQILXSA-N
Smiles	CC1=NN=C2[C@H](CC(=O)NCCCCCCCCNC(=O)COC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)N=C(C3=C(SC(C)=C3C)N12)C1=CC=C(Cl)C=C1
E3 ligase	CRBN
DC₅₀ / D_max	6 nM / 97% - Degradation of BRD4 in HEK293T cells after 3 h treatment
K_d (Degrader to Target)	46 nM - K_d of BRD4 BD1 was assessed by FP
Selectivity confirmed by global proteomics	Yes

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 dBET6

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	84.14	100

Preparing Stock Solutions for dBET6

The following data is based on the product molecular weight 841.38.

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	1.19 mL	5.94 mL	11.89 mL
5 mM	0.24 mL	1.19 mL	2.38 mL
10 mM	0.12 mL	0.59 mL	1.19 mL
50 mM	0.02 mL	0.12 mL	0.24 mL

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References for dBET6

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

Verstovsek Targeting cistrome and dysregulated transcriptome of post-MPN sAML. Oncotarget 2017 PMID: 29212143
Nowak Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat.Chem.Biol. 2018 PMID: 29892083
Winter BET Bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol. Cell 2017 PMID: 28673542