NU 9056 |
Catalog No.GC11972
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1450644-28-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 1450644-28-6 | SDF | |
| Chemical Name | 1,2-di(isothiazol-5-yl)disulfane | ||
| Canonical SMILES | C1(SSC2=CC=NS2)=CC=NS1 | ||
| Formula | C6H4N2S4 | M.Wt | 232.37 |
| Solubility | <10mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3035 mL | 21.5174 mL | 43.0348 mL |
| 5 mM | 860.7 μL | 4.3035 mL | 8.607 mL |
| 10 mM | 430.3 μL | 2.1517 mL | 4.3035 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A liquid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)