| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
KAT5 (Tip60, Lysine Acetyltransferase 5).
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|---|---|
| ln Vitro |
In a concentration- and time-dependent manner, NU9056 (17–36 μM; 24-96 hours) activates caspase 3 and 9. The cue histones H4K16, H3K14, and H4K8, which are the targets of Tip60-mediated oralization, are less abundant after treatment with NU9056 (2.5–40 μM; 2) [1]. A treatment with NU9056 also decreased the levels of p53 and p21 proteins, drought stress front, and androgen irrigation [1].
NU-9056 inhibits KAT5 with an IC50 of <2 uM, showing selectivity over other HATs: IC50 values are 60 uM for p300, 36 uM for pCAF, and >100 uM for GCN5. In prostate cancer cell lines, it inhibits protein acetylation, blocks DNA damage response, and reduces LNCaP cell proliferation in a concentration- and time-dependent manner. |
| ln Vivo |
Mice were injected with Nu9056 (2 μg/g), and hippocampi were harvested 1 hour later. Tip60 inhibits H2A.Z binding on the -1 nucleosome of Arc and the +1 nucleosome of Arc and Syp. In addition, Nu9056 promotes the throating of -1 nucleosomes of Fos, Tacstd2 and Gria4 as well as the +1 nucleosome of Gria4 [2].
Cellular and animal studies: In LPS-treated mice, NU-9056 improves survival, alleviates cognitive impairment, anxiety, and depression; it also inhibits cardiac fibrosis and improves cardiac remodeling post-myocardial infarction; in anaplastic thyroid carcinoma (ATC) models, it suppresses tumor proliferation via the c-Myc/miR-202 pathway. |
| Enzyme Assay |
KAT5 enzymatic activity is measured in cell-free assays using recombinant KAT5 enzyme and biotinylated histone H4 peptide substrate; after incubation with NU-9056 and acetyl-CoA, acetylation is detected by ELISA or Western blot using specific anti-acetylated H4K16 antibodies; IC50 values are calculated from dose-response curves.
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: LNCaP Cell Tested Concentrations: 17 µM, 24 µM, 36 µM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours), 96 hrs (hours) Experimental Results: Induction of apoptosis by activating caspase 3 and caspase 9 at a certain concentration and time Dependence on death. Western Blot Analysis[1] Cell Types: LNCaP Cell Tested Concentrations: 2.5 µM, 5 µM, 10 µM, 20 µM, 40 µM Incubation Duration: 2 hrs (hours) Experimental Results: diminished levels of Tip60 target acetylated histones H4K16, H3K14 and H4K8 - mediator induced acetylation. Cell lines (e.g., LNCaP prostate cancer, anaplastic thyroid carcinoma cells) are cultured in RPMI-1640 or DMEM medium with 10% FBS; cells are treated with NU-9056 (17-36 uM, 24-96 hours); cell viability is measured by CCK-8 or MTT assays; protein acetylation is assessed by Western blot; apoptosis is evaluated by caspase 3/9 activation and flow cytometry. |
| Animal Protocol |
Mouse models include LPS-induced systemic inflammation, myocardial infarction (MI), and anaplastic thyroid carcinoma xenografts; NU-9056 is administered via intraperitoneal injection (typical dose: 2 ug/g); endpoints include survival rate, behavioral tests, cardiac function (echocardiography), tumor volume, and molecular analysis of target pathway markers.
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| ADME/Pharmacokinetics |
PK properties not fully detailed; limited information on absorption and systemic exposure; as a small-molecule inhibitor, further ADME studies are required to determine half-life, plasma clearance, oral bioavailability, and tissue distribution; microsomal stability data are not publicly available.
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| Toxicity/Toxicokinetics |
Toxicity profile not fully characterized; in animal studies (mice), NU-9056 appears to be tolerated at the tested doses without overt signs of toxicity; formal acute and repeat-dose toxicity studies are lacking; as an experimental compound, its safety profile for human use has not been established.
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| References | |
| Additional Infomation |
Structure in the first source
NU-9056 is a research-use only compound for studying KAT5/Tip60 function in acetylation-dependent cellular processes, including DNA damage response, cancer biology, and cardiac fibrosis; it has not been approved by FDA or EMA; no clinical trials have been registered; it is a valuable tool for epigenetic research and validation of KAT5 as a therapeutic target. |
| Molecular Formula |
C6H4N2S4
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|---|---|
| Molecular Weight |
232.35
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| Exact Mass |
231.925
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| CAS # |
1450644-28-6
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| PubChem CID |
72201043
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| Appearance |
Yellow to brown liquid
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
209.2±40.0 °C at 760 mmHg
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| Flash Point |
80.3±27.3 °C
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| Vapour Pressure |
0.3±0.4 mmHg at 25°C
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| Index of Refraction |
1.759
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| LogP |
1.59
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
130
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=CC=NS1)SC1=CC=NS1
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| InChi Key |
MLRAMCAHIWHWRM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H4N2S4/c1-3-7-9-5(1)11-12-6-2-4-8-10-6/h1-4H
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| Chemical Name |
5-(1,2-thiazol-5-yldisulfanyl)-1,2-thiazole
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| Synonyms |
NU-9056 NU 9056 NU9056
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~537.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 1.1 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3039 mL | 21.5193 mL | 43.0385 mL | |
| 5 mM | 0.8608 mL | 4.3039 mL | 8.6077 mL | |
| 10 mM | 0.4304 mL | 2.1519 mL | 4.3039 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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