Merck, 5005110001, Histone Acetyltransferase Inhibitor VIII, NU9056

General description
NU9056, a disulfane compound, is reported to be a potent inhibitor of lysine acetyltransferase 5 (KAT5). NU9056 inhibits protein acetylation in prostate cancer cell lines. It acts against histone acetyltransferase KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100 µM, respectively) and effectively reduces H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µM). Shown to induce cell cycle arrest and apoptosis (17 to 24 µM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
KAT5
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)