GLPBio

NU 9056

Catalog No.: GC11972Purity:>98.00%
COASDSData Sheet
NU 9056 (1,2-bis(isothiazol-5-yl) disulfide) is a potent and selective Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor with an IC50 value of 2μM and anti-tumor activity.

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NU 9056
Cas No.: 1450644-28-6
10mM (in 1mL DMSO)In Stock
$108.00
1
1mgIn Stock
$50.00
1
5mgIn Stock
$98.00
1
10mgIn Stock
$157.00
1
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Description

NU 9056 (1,2-bis(isothiazol-5-yl) disulfide) is a potent and selective Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor with an IC50 value of 2μM and anti-tumor activity[1, 2]. Tip60 regulates key biological processes such as gene transcription, DNA damage repair, and cell apoptosis by acetylation of histones (such as H4, H2A) and non-histone substrates[3]. NU 9056 is more than 16 times more selective for Tip60 than PCAF, p300, and GCN5[4].

In vitro, NU 9056 (2.5-40μM) treated human anaplastic thyroid carcinoma (ATC) cells (CAL-62 cells) for 48h effectively inhibited ATC cell proliferation in a concentration-dependent manner, reduced the expression levels of intracellular acetyl histone H2A and acetyl histone H4, and inhibited cell migration, invasion, and tube formation[5].

In vivo, NU 9056 (5mg/kg) treated with intraperitoneal injection in mice with lipopolysaccharide (LPS)-induced sepsis-associated encephalopathy (SAE) improved the survival rate of mice and alleviated cognitive impairment, anxiety, and depressive behaviors[6].

References:
[1] Coffey K, Blackburn T J, Cook S, et al. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer[J]. 2012.
[2] Xu L, Qin Y, Liu M, et al. The acetyltransferase KAT5 inhibitor NU 9056 promotes apoptosis and inhibits JAK2/STAT3 pathway in Extranodal NK/T cell lymphoma[J]. Anti-Cancer Agents in Medicinal Chemistry-Anti-Cancer Agents), 2022, 22(8): 1530-1540.
[3] Lashgari A, Tchara P E K, Lambert J P, et al. New insights into the DNA repair pathway choice with NuA4/TIP60[J]. DNA repair, 2022, 113: 103315.
[4] Dansu D K. Changes in the Epigenetic Landscape of Oligodendrocyte Progenitor Cells With Time[D]. City University of New York, 2023.
[5] Xu W, Xie L, Yang Y, et al. KAT5 Inhibitor NU9056 Suppresses Anaplastic Thyroid Carcinoma Progression through c‐Myc/miR‐202 Pathway[J]. International journal of endocrinology, 2022, 2022(1): 2014568.
[6] Chen L, Qing W, Yi Z, et al. NU9056, a KAT 5 inhibitor, treatment alleviates brain dysfunction by inhibiting NLRP3 inflammasome activation, affecting gut microbiota, and derived metabolites in LPS-treated mice[J]. Frontiers in Nutrition, 2021, 8: 701760.

Protocol

Cell experiment [1]:

Cell lines

Human Anaplastic thyroid carcinoma (ATC) cells ( CAL-62 cells)

Preparation Method

Cells were plated into 96-well plates (4×103 cells/well), cultured overnight, and treated with NU 9056 (2.5-40μM) for 48h. Then, CCK-8 solution was added and incubated for 2h at 37°C. Next, the OD value was measured using a microplate reader at a wavelength of 450nm.

Reaction Conditions

2.5-40μM; 48h

Applications

NU 9056 potently inhibited ATC cell proliferation in a concentration-dependent manner.

Animal experiment [2]:

Animal models

C57BL/6 J mice

Preparation Method

Ninety-five, 12-week-old C57BL/6J mice weighing 25-30g were randomly divided into a control group, a lipopolysaccharide (LPS) group, and an NU 9056 (LPS+NU 9056) group. LPS-treated mice received an intraperitoneal injection of LPS (10mg/kg). Control mice were injected with the same amount of normal saline. NU 9056 (5mg/kg) was intraperitoneally injected twice, 30min before and 24h after LPS injection. Sixteen hours after intraperitoneal injection of LPS, blood was collected transcardially. The supernatant was separated and collected. The experiment was performed immediately. Finally, the remaining samples were stored at -80°C. Another 43 mice were randomly divided into three groups with the same grouping and treatment methods as well as before. The animal survival rate and behavioral experiments were carried out. The mice were euthanized by intraperitoneal injection of sodium pentobarbital 150mg/kg.

Dosage form

5mg/kg; i.p.

Applications

NU 9056 improved the survival rate of mice and alleviated LPS-induced cognitive impairment, anxiety, and depression in vivo.

References:
[1] Xu W, Xie L, Yang Y, et al. KAT5 Inhibitor NU9056 Suppresses Anaplastic Thyroid Carcinoma Progression through c?Myc/miR?202 Pathway[J]. International journal of endocrinology, 2022, 2022(1): 2014568.
[2]Chen L, Qing W, Yi Z, et al. NU9056, a KAT 5 inhibitor, treatment alleviates brain dysfunction by inhibiting NLRP3 inflammasome activation, affecting gut microbiota, and derived metabolites in LPS-treated mice[J]. Frontiers in Nutrition, 2021, 8: 701760.

Product Documents

Purity:>98.00%Appearance:A liquid
COASDSData Sheet

Chemical Properties

CAS No.
1450644-28-6
Chemical Name
1,2-di(isothiazol-5-yl)disulfane
SMILES
C1(SSC2=CC=NS2)=CC=NS1
Molecular Formula
C6H4N2S4
Molecular Weight
232.37
Solubility
<10mg/ml in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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