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DBr-1

Chemical Structure : DBr-1

CAS No.:

DBr-1 (DCAF1-BRD9 PROTAC)

Catalog No.: PC-21642Not For Human Use, Lab Use Only.

DBr-1 (DCAF1-BRD9 PROTAC) is a potent, selective DCAF1-BRD9 PROTAC (DC50=90 nM, HEK293) by coupling the BRD9 bromodomain binder BI-9564 via a piperidine and aliphatic carbon linker to the piperazine of DCAF1 binder.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DBr-1 (DCAF1-BRD9 PROTAC) is a potent, selective DCAF1-BRD9 PROTAC (DC50=90 nM, HEK293) by coupling the BRD9 bromodomain binder BI-9564 via a piperidine and aliphatic carbon linker to the piperazine of DCAF1 binder.
DBr-1 shows a similar degradation preference as the CRBN-based PROTAC dBRD9, only strongly affecting BRD9 but unlike the VZ185 not BRD7 levels.
DBr-1 potently degrades BRD9 with a DC50 of 90 nM but only weakly affected BRD7 protein levels in HEK293/BRD9-HiBiT and HEK293/BRD7-HiBiT cells, respectively.

Physicochemical Properties

M.Wt 970.66
Formula C55H68ClN9O5
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

4-(4-((4-((6-(4-(4-((2-aminoethyl)amino)-2-(1-(4-chlorophenyl)cyclohexyl)quinazolin-7-yl)piperazin-1-yl)-6-oxohexyl)oxy)piperidin-1-yl)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

References

1. Schröder M, et al. Nat Commun. 2024 Jan 4;15(1):275.

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