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Beschreibung

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 µ,M, respectively) and effectively reduce H3K14, H4K8, H4K16, but not alpha-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µ,M). Shown to induce cell cycle arrest and apoptosis (17 to 24 µ,M) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27 µ,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., 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 µ,M, respectively) and effectively reduce H3K14, H4K8, H4K16, but not alpha-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µ,M, 2 µ,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 µ,M and 12%/23%/25%/92%/24 µ,M) and apoptosis (fold caspase-9 cleavage increase/dose in 24 h = 2.5/17 µ,M & 3.5/24 µ,M, fold caspase-3 cleavage increase/dose in 96 h = 6.3/17 µ,M & 11/24 µ,M) 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 µ,M, respectively, against WR22rvl, LNCaP-CdxR, LNCaP-AI, LNCaP, and PC3 cells).

Strukturformel

SAF-5005110001

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