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Submit ReviewdBET6
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)
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
| E3 ligase | CRBN |
| DC50 / Dmax | 6 nM / 97% - Degradation of BRD4 in HEK293T cells after 3 h treatment |
| Kd (Degrader to Target) | 46 nM - Kd of BRD4 BD1 was assessed by FP |
| Selectivity confirmed by global proteomics | Yes |
| 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 |
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 Data for dBET6
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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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Product Datasheets for dBET6
References for dBET6
References are publications that support the biological activity of the product.
Winter et al (2017) BET Bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol. Cell 67 5 PMID: 28673542
Verstovsek et al (2017) Targeting cistrome and dysregulated transcriptome of post-MPN sAML. Oncotarget 8 93301 PMID: 29212143
Nowak et al (2018) Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat.Chem.Biol. 14 706 PMID: 29892083
If you know of a relevant reference for dBET6, please let us know.
View Related Products by Target
Keywords: dBET6, dBET6 supplier, Potent, selective, active, degraders, degrades, BET, bromodomains, BRD4, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, degradation, JQ1, cell, permeable, in, vivo, tpd, Active, Degraders, Bromodomains, 6945, Tocris Bioscience
Citations for dBET6
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Epigenetics Scientific Review
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Epigenetics in Cancer PosterUpdated
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia