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Active Degraders Small Molecule
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Description: Potent and selective BRD9 degrading PROTAC

Chemical Name: 2-[[[4-(1,2-Dihydro-2-methyl-1-oxo-2,7-naphthyridin-4-yl)-2-6-dimethoxyphenyl]methyl]methylamino]-N-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide dihydrochloride

Purity: ≥98%

Product Details

Biological Activity

PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide (Cat. No. 6302). Potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). Does not degrade BRD4 or BRD7 at concentrations up to 5 μM. Displays antiproliferative effects in human AML cell lines.

Technical Data

Soluble to 20 mM in water and to 50 mM in DMSO
Store at -20°C

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.

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute.

Background References

  1. Degradation of the BAF complex factor BRD9 by heterobifunctional ligands.
    Remillard et al.
    Angew.Chem.Int.Ed.Engl., 2017;56:5738

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