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5.00511

Histone Acetyltransferase Inhibitor VIII, NU9056

Synonym(e):

Histone Acetyltransferase Inhibitor VIII, NU9056, HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V, 1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I

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PackungsgrößeSKUVerfügbarkeitPreis
10 mg
Warenkorb auf Verfügbarkeit prüfen
€ 243,00

Über diesen Artikel

Empirische Formel (Hill-System):
C6H4N2S4
CAS-Nummer:
Molekulargewicht:
232.37
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
oil
Storage condition:
OK to freeze, protect from light

€ 243,00


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assay

≥97% (HPLC)

Quality Segment

form

oil

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow-brown

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

SMILES string

[s]1nccc1SSc2[s]ncc2

InChI

1S/C6H4N2S4/c1-3-7-9-5(1)11-12-6-2-4-8-10-6/h1-4H

InChI key

MLRAMCAHIWHWRM-UHFFFAOYSA-N

General description

NU9056, a disulfane compound, is reported to be a potent inhibitor of lysine acetyltransferase 5 (KAT5). NU9056 inhibits protein acetylation in prostate cancer cell lines. It acts against histone acetyltransferase KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100 µM, respectively) and effectively reduces H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µM). Shown to induce cell cycle arrest and apoptosis (17 to 24 µM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27 µM).[1]

Biochem/physiol Actions

Cell permeable: yes
Primary Target
KAT5
Reversible: yes

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Dieser Artikel
382175-M5.09703218860
form

oil

form

solid

form

solid

form

solid

assay

≥97% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

≥99% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light


Lagerklasse

10 - Combustible liquids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



Analysenzertifikate (COA)

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Verwandter Inhalt

Cancer is a complex disease manifestation. At its core, it remains a disease of abnormal cellular proliferation and inappropriate gene expression. In the early days, carcinogenesis was viewed simply as resulting from a collection of genetic mutations that altered the gene expression of key oncogenic genes or tumor suppressor genes leading to uncontrolled growth and disease (Virani, S et al 2012). Today, however, research is showing that carcinogenesis results from the successive accumulation of heritable genetic and epigenetic changes. Moreover, the success in how we predict, treat and overcome cancer will likely involve not only understanding the consequences of direct genetic changes that can cause cancer, but also how the epigenetic and environmental changes cause cancer (Johnson C et al 2015; Waldmann T et al 2013). Epigenetics is the study of heritable gene expression as it relates to changes in DNA structure that are not tied to changes in DNA sequence but, instead, are tied to how the nucleic acid material is read or processed via the myriad of protein-protein, protein-nucleic acid, and nucleic acid-nucleic acid interactions that ultimately manifest themselves into a specific expression phenotype (Ngai SC et al 2012, Johnson C et al 2015). This review will discuss some of the principal aspects of epigenetic research and how they relate to our current understanding of carcinogenesis. Because epigenetics affects phenotype and changes in epigenetics are thought to be key to environmental adaptability and thus may in fact be reversed or manipulated, understanding the integration of experimental and epidemiologic science surrounding cancer and its many manifestations should lead to more effective cancer prognostics as well as treatments (Virani S et al 2012).






Global Trade Item Number

SKUGTIN
500511000104055977245738

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