NU-9056 | CAS# 1450644-28-6 | KAT5 (Tip60) histone acetyltransferase inhibitor

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

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
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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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	comments
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.

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:

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

View History

CHR-090

MedKoo CAT#: 530555

CAS#: 728865-23-4