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dBET6

Chemical Structure : dBET6

CAS No.: 1950634-92-0

dBET6 (dBET 6)

Catalog No.: PC-61699Not For Human Use, Lab Use Only.

dBET6 is a highly potent, cell-permeable, optimized chemical degrader of BET bromodomain BRD4 with IC50 of 14 nM.

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Purity & Documentation Purity: 98.46% (HPLC) Select Batch:

Biological Activity

dBET6 is a highly potent, cell-permeable, optimized chemical degrader of BET bromodomain BRD4 with IC50 of 14 nM.
dBET6 (100 nM) leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis in in T-ALL cells (MOLT4).
dBET6 prompts a collapse of global elongation that phenocopies CDK9 inhibition.

Physicochemical Properties

M.Wt 841.381
Formula C42H45ClN8O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 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-, (6S)-

References

1. Winter GE, et al. Mol Cell. 2017 Jul 6;67(1):5-18.e19.

2. Cancer Discov. 2017 Aug;7(8):794.

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