5.00511

Histone Acetyltransferase Inhibitor VIII, NU9056

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₆H₄N₂S₄
• Molecular Weight: 232.37

Properties

• Assay: ≥97% (HPLC)
• Quality Level: 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

Description

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). 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).

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 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

Primary Target
KAT5

Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable