Histone Acetyltransferase Inhibitor VIII, NU9056-Calbiochem

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一般描述

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 ?M, respectively) and effectively reduce H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 ?M; 2 ?M 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 ?M and 12%/23%/25%/92%/24 ?M) and apoptosis (fold caspase-9 cleavage increase/dose in 24 h = 2.5/17 ?M & 3.5/24 ?M; fold caspase-3 cleavage increase/dose in 96 h = 6.3/17 ?M & 11/24 ?M) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI₅₀in three doubling time = 7.5, 12, 16, 24, and 27 ?M, respectively, against WR22rvl, LNCaP-CdxR, LNCaP-AI, LNCaP, and PC3 cells).
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 ?M, respectively) and effectively reduce H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 ?M). Shown to induce cell cycle arrest and apoptosis (17 to 24 ?M) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI₅₀from 7.5 to 27 ?M).

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.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
KAT5

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Coffey, K., et al. 2012.PLoS One.7,e45539.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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安全信息