1. Epigenetics Apoptosis
  2. Histone Acetyltransferase Apoptosis
  3. NU9056

NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.

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NU9056 Chemical Structure

NU9056 Chemical Structure

CAS No. : 1450644-28-6

Size Price Stock Quantity
Liquid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 275 In-stock
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Liquid
1 mg USD 90 In-stock
5 mg USD 250 In-stock
10 mg USD 370 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an [1][2] of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells[1].

In Vitro

NU9056 (17-36 µM; 24-96 hours) results in both caspase 3 and caspase 9 activation in a time- and concentration-dependent manner[1].
NU9056 (2.5-40 µM; 2 hours) treatment results in decreased levels of acetylated histone H4K16, H3K14 and H4K8, targets for Tip60-mediated acetylation[1].
NU9056 treatment also decreases androgen receptor, prostate specific antigen, p53 and p21 protein levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: LNCaP cells
Concentration: 17 µM, 24 µM, 36 µM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Induced apoptosis via activation of caspase 3 and caspase 9 in a concentration- and time-dependent manner.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 2.5 µM, 5 µM, 10 µM, 20 µM, 40 µM
Incubation Time: 2 hours
Result: Resulted in decreased levels of acetylated histone H4K16, H3K14 and H4K8, targets for Tip60-mediated acetylation.
In Vivo

The mice are injected with Nu9056 (2 μg/g) and the hippocampus is collected 1 h later. Tip60 inhibition reduces H2A.Z binding at the -1 nucleosome of Arc, and the +1 nucleosome of Arc and Syp. Additionally, Nu9056 increases acetylation at the -1 nucleosome of Fos, Tacstd2, and Gria4, and the +1 nucleosome of Gria4[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

232.37

Formula

C6H4N2S4

CAS No.
Appearance

Liquid

Color

Yellow to brown

SMILES

C1(SSC2=CC=NS2)=CC=NS1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (537.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3035 mL 21.5174 mL 43.0348 mL
5 mM 0.8607 mL 4.3035 mL 8.6070 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (8.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (8.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.81%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3035 mL 21.5174 mL 43.0348 mL 107.5870 mL
5 mM 0.8607 mL 4.3035 mL 8.6070 mL 21.5174 mL
10 mM 0.4303 mL 2.1517 mL 4.3035 mL 10.7587 mL
15 mM 0.2869 mL 1.4345 mL 2.8690 mL 7.1725 mL
20 mM 0.2152 mL 1.0759 mL 2.1517 mL 5.3794 mL
25 mM 0.1721 mL 0.8607 mL 1.7214 mL 4.3035 mL
30 mM 0.1434 mL 0.7172 mL 1.4345 mL 3.5862 mL
40 mM 0.1076 mL 0.5379 mL 1.0759 mL 2.6897 mL
50 mM 0.0861 mL 0.4303 mL 0.8607 mL 2.1517 mL
60 mM 0.0717 mL 0.3586 mL 0.7172 mL 1.7931 mL
80 mM 0.0538 mL 0.2690 mL 0.5379 mL 1.3448 mL
100 mM 0.0430 mL 0.2152 mL 0.4303 mL 1.0759 mL
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NU9056 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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NU9056
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HY-110127
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