BRD8 inhibitor DN02

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Chemical Structure : BRD8 inhibitor DN02

CAS No.: 3055009-00-9

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

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.
BRD8 inhibitor DN02 displays IC50 of 0.64 uM in-cell engagement within BRET displacement assays.
BRD8 inhibitor DN02 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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