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 >100uM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not alpha-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10uM). Shown to induce cell cycle arrest and apoptosis (17 to 24uM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27uM).
Synonyms:HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V, 1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I
Solubility:≥50mg/ml (DMSO)
Molecular Formula:C₆H₄N₂S₄
Primary Target:KAT5
Method for Determining Identity:Proton NMR Spectroscopic and Mass Spectrometric analysis
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. Aliquots are stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.