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

NU9056 

Cat. No.: HY-110127
Handling Instructions

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.

For research use only. We do not sell to patients.

NU9056 Chemical Structure

NU9056 Chemical Structure

CAS No. : 1450644-28-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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

Molecular Weight

232.37

Formula

C₆H₄N₂S₄

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (537.94 mM; Need ultrasonic)

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
10 mM 0.4303 mL 2.1517 mL 4.3035 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

*All of the co-solvents are provided by MCE.
References
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Keywords:

NU9056NU 9056NU-9056Histone AcetyltransferaseApoptosisHATsHATTip60KAT5apoptosisprostatecanceracetylationInhibitorinhibitorinhibit

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NU9056
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HY-110127
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