dBET6
Tocris Bioscience, part of Bio-Techne | Catalog # 6945
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
Product Description
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 InstituteProduct Specifications
Molecular Weight
841.38
Formula
C42H45ClN8O7S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for dBET6
For research use only
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