Histone Acetyltransferase Inhibitor VIII, NU9056 - Calbiochem

General Description

A cell-permeable disulfane compound that is reported to be more potent against KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC₅₀ ≤2, ≤36, ≤60, and >100 μM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 μM; 2 μM TSA, Cat. No. 647925, added in the last 4 h of 6 h NU9056 treatment to block HDAC activity). Shown to induce cell cycle arrest (% subG1 population after 24 h/48 h/72 h/ 96 h/dose = 9.3%/15%/22%/61%/17 μM and 12%/23%/25%/92%/24 μM) and apoptosis (fold caspase-9 cleavage increase/dose in 24 h = 2.5/17 μM & 3.5/24 μM; fold caspase-3 cleavage increase/dose in 96 h = 6.3/17 μM & 11/24 μM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI₅₀ in three doubling time = 7.5, 12, 16, 24, and 27 μM, respectively, against WR22rvl, LNCaP-CdxR, LNCaP-AI, LNCaP, and PC3 cells).

Biochem/physiol Actions

Cell permeable: yes

Raw materials

Preparation Products