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BRD8 inhibitor DN02

Chemical Structure : BRD8 inhibitor DN02

CAS No.:

BRD8 inhibitor DN02

Catalog No.: PC-72321Not For Human Use, Lab Use Only.

BRD8 inhibitor DN02 is a first-in-class selective and cellularly active probe for NuA4 factor BRD8 (BD1) with AlphaScreen IC50 of 48 nM, and Kd of 34 nM, displays IC50 of 0.64 uM in-cell engagement within BRET displacement assays, shows no affinity for BRD8 (BD2), CBP, and p300 (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BRD8 inhibitor DN02 is a first-in-class selective and cellularly active probe for NuA4 factor BRD8 (BD1) with AlphaScreen IC50 of 48 nM, and Kd of 34 nM, displays IC50 of 0.64 uM in-cell engagement within BRET displacement assays, shows no affinity for BRD8 (BD2), CBP, and p300 (IC50>10 uM).

Physicochemical Properties

M.Wt 397.450
Formula C22H24FN3O3
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-((3-aminoazetidin-1-yl)methyl)-2,6-dimethoxyphenyl)-7-fluoro-2-methylisoquinolin-1(2H)-one

References

1. David Remillard, et al. ACS Chem Biol. 2021 Nov 19;16(11):2185-2192.

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