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MedKoo Cat#: 574820 | Name: NU-9056
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NU-9056 is a selective KAT5 (Tip60) histone acetyltransferase inhibitor that inhibits protein acetylation in prostate cancer cell lines and blocks DNA damage response. NU-9056 also decreases proliferation of LNCaP cells and induces apoptosis via caspase activation.

Chemical Structure

NU-9056
NU-9056
CAS#1450644-28-6

Theoretical Analysis

MedKoo Cat#: 574820

Name: NU-9056

CAS#: 1450644-28-6

Chemical Formula: C6H4N2S4

Exact Mass: 231.9257

Molecular Weight: 232.35

Elemental Analysis: C, 31.02; H, 1.74; N, 12.06; S, 55.19

Price and Availability

Size Price Availability Quantity
5mg USD 235.00 2 Weeks
10mg USD 385.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 940.00 2 Weeks
100mg USD 1,385.00 2 Weeks
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Related CAS #
No Data
Synonym
NU-9056; NU 9056; NU9056
IUPAC/Chemical Name
5-(1,2-Thiazol-5-yldisulfanyl)-1,2-thiazole
InChi Key
MLRAMCAHIWHWRM-UHFFFAOYSA-N
InChi Code
InChI=1S/C6H4N2S4/c1-3-7-9-5(1)11-12-6-2-4-8-10-6/h1-4H
SMILES Code
C1(SSC2=CC=NS2)=CC=NS1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor.
In vitro activity:
Although an authentic sample of 4-methyl-5-bromoisothiazole was inactive against Tip60, in an in vitro HAT assay, 1,2-bis(isothiazol-5-yl)disulfane (NU9056) was identified as a relatively potent inhibitor (IC(50) 2 µM). NU9056 treatment inhibited cellular proliferation in a panel of prostate cancer cell lines (50% growth inhibition, 8-27 µM) and induced apoptosis via activation of caspase 3 and caspase 9 in a concentration- and time-dependent manner. Reference: PLoS One. 2012;7(10):e45539. https://pubmed.ncbi.nlm.nih.gov/23056207/
In vivo activity:
NU9056 improved the survival rate of mice and alleviated LPS-induced cognitive impairment, anxiety, and depression in vivo. The tight junctions were thickened via NU9056 treatment. Further, the mRNAs and proteins expression levels of Occludin and Claudin 5 were up-regulated by NU9056. NU9056 increased the expression level of DCX. The expression levels of Iba-1, NLRP3, IL-1β, ASC, and Casp-1 P10 were down-regulated by NU9056. The composition of the gut microbiota changed. Reference: Front Nutr. 2021 Jul 13;8:701760. https://pubmed.ncbi.nlm.nih.gov/34327209/
Solvent mg/mL mM
Solubility
DMSO 125.0 537.98
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 232.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Narkaj K, Stefanelli G, Wahdan M, Azam AB, Ramzan F, Steininger CFD Jr, Walters BJ, Zovkic IB. Blocking H2A.Z Incorporation via Tip60 Inhibition Promotes Systems Consolidation of Fear Memory in Mice. eNeuro. 2018 Nov 8;5(5):ENEURO.0378-18.2018. doi: 10.1523/ENEURO.0378-18.2018. PMID: 30417078; PMCID: PMC6223110. 2. Coffey K, Blackburn TJ, Cook S, Golding BT, Griffin RJ, Hardcastle IR, Hewitt L, Huberman K, McNeill HV, Newell DR, Roche C, Ryan-Munden CA, Watson A, Robson CN. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One. 2012;7(10):e45539. doi: 10.1371/journal.pone.0045539. Epub 2012 Oct 8. PMID: 23056207; PMCID: PMC3466219. 3. Chen L, Qing W, Yi Z, Lin G, Peng Q, Zhou F. NU9056, a KAT 5 Inhibitor, Treatment Alleviates Brain Dysfunction by Inhibiting NLRP3 Inflammasome Activation, Affecting Gut Microbiota, and Derived Metabolites in LPS-Treated Mice. Front Nutr. 2021 Jul 13;8:701760. doi: 10.3389/fnut.2021.701760. PMID: 34327209; PMCID: PMC8313765.
In vitro protocol:
1. Narkaj K, Stefanelli G, Wahdan M, Azam AB, Ramzan F, Steininger CFD Jr, Walters BJ, Zovkic IB. Blocking H2A.Z Incorporation via Tip60 Inhibition Promotes Systems Consolidation of Fear Memory in Mice. eNeuro. 2018 Nov 8;5(5):ENEURO.0378-18.2018. doi: 10.1523/ENEURO.0378-18.2018. PMID: 30417078; PMCID: PMC6223110. 2. Coffey K, Blackburn TJ, Cook S, Golding BT, Griffin RJ, Hardcastle IR, Hewitt L, Huberman K, McNeill HV, Newell DR, Roche C, Ryan-Munden CA, Watson A, Robson CN. Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One. 2012;7(10):e45539. doi: 10.1371/journal.pone.0045539. Epub 2012 Oct 8. PMID: 23056207; PMCID: PMC3466219.
In vivo protocol:
1. Chen L, Qing W, Yi Z, Lin G, Peng Q, Zhou F. NU9056, a KAT 5 Inhibitor, Treatment Alleviates Brain Dysfunction by Inhibiting NLRP3 Inflammasome Activation, Affecting Gut Microbiota, and Derived Metabolites in LPS-Treated Mice. Front Nutr. 2021 Jul 13;8:701760. doi: 10.3389/fnut.2021.701760. PMID: 34327209; PMCID: PMC8313765.
1. Coffey et al (2012) Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One 7 e45539 PMID: 23056207

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