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Merck

SML3018

Sigma-Aldrich

TH1834

≥98% (HPLC)

Sinónimos:

2-(5-(4-((Phenethyl(4-(4-(pyrrolidin-1-ylmethyl)phenoxy)butyl)amino)methyl)phenyl)-2H-tetrazol-2-yl)acetic acid dihydrochloride, 2H-Tetrazole-2-acetic acid, 5-[4-[[(2-phenylethyl)[4-[4-(1-pyrrolidinylmethyl)phenoxy]butyl]amino]methyl]phenyl]-, hydrochloride (1:2), TIP60i

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About This Item

Fórmula empírica (notación de Hill):
C33H40N6O3 · 2HCl
Número de CAS:
Peso molecular:
641.63
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

O=C(O)CN1N=C(C2=CC=C(CN(CCC3=CC=CC=C3)CCCCOC4=CC=C(CN5CCCC5)C=C4)C=C2)N=N1.[H]Cl.[H]Cl

Biochem/physiol Actions

TH1834 is a cell penetrant, potent and selective histone acetyltransferase (HAT) Tip60 inhibitor that interact with active binding pocket of Tip60. TH1834 induces apoptosis and increased unrepaired DNA damage in breast and prostate cancer cell lines but not control MCF10A cells.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificados de análisis (COA)

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James A L Brown et al.
Biochemical Society transactions, 44(4), 979-986 (2016-08-17)
Two opposing enzyme classes regulate fundamental elements of genome maintenance, gene regulation and metabolism, either through addition of an acetyl moiety by histone acetyltransferases (HATs) or its removal by histone de-acetyltransferases (HDAC), and are exciting targets for drug development. Importantly
Mouhamed Idrissou et al.
Omics : a journal of integrative biology, 24(10), 581-591 (2020-09-23)
Breast cancer is often sporadic due to several factors. Among them, the deregulation of epigenetic proteins may be involved. TIP60 or KAT5 is an acetyltransferase that regulates gene transcription through the chromatin structure. This pleiotropic protein acts in several cellular
Chunxia Gao et al.
Scientific reports, 4, 5372-5372 (2014-06-21)
Histone acetylation is required for many aspects of gene regulation, genome maintenance and metabolism and dysfunctional acetylation is implicated in numerous diseases, including cancer. Acetylation is regulated by histone acetyltransferases (HATs) and histone deacetylases and currently, few general HAT inhibitors

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