5.00511

Histone Acetyltransferase Inhibitor VIII, NU9056

• Synonym(e): Histone Acetyltransferase Inhibitor VIII, NU9056, 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
• Empirische Formel (Hill-System): C₆H₄N₂S₄
• CAS-Nummer: 1450644-28-6
• Molekulargewicht: 232.37
• MDL number: MFCD26792588
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: oil
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥97% (HPLC)
• Quality Segment: 100
• form: oil
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow-brown
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• SMILES string: [s]1nccc1SSc2[s]ncc2
• InChI: 1S/C6H4N2S4/c1-3-7-9-5(1)11-12-6-2-4-8-10-6/h1-4H
• InChI key: MLRAMCAHIWHWRM-UHFFFAOYSA-N

Beschreibung

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)

Sicherheitshinweise

• Lagerklasse: 10 - Combustible liquids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable