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Oxamflatin

Catalog No.
B7796
HADC inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$203.00
Ship with 10-15 days
1mg
$90.00
Ship with 10-15 days
5mg
$270.00
Ship with 10-15 days
10mg
$420.00
Ship with 10-15 days
25mg
$915.00
Ship with 10-15 days

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Email: [email protected]

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Background

Oxamflatin is a potent histone deacetylase inhibitor with IC50 value of 15.7 nM [1].

Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.

Oxamflatin is a potent histone deacetylase inhibitor and a novel antitumor compound. In mouse and human tumor cell lines, such as P388, Lewis, Lu-99, HT-29 and HeLa cells, Oxamflatin exhibited antiproliferative activity. In HeLa cells, Oxamflatin changed cell morphology, and significantly reduced the number of the cells in S phase and increased the number of cells in G0/G1 phase [1]. In the HIV-1 latently infected Jurkat T cell line, Oxam?atin increased the acetylation level of histone H3 and histone H4 at the nucleosome 1(nuc-1) site of the HIV-1 LTR and activated HIV-1 gene expression by 2-17 fold, suggesting that Oxam?atin has potential as drug candidates as antilatency therapies [2]. In OVCAR-5 and SKOV-3 ovarian cancer cell lines, oxamflatin decreased cell viability and significantly inhibited DNA synthesis and cell proliferation. Also, oxamflatin reduced the expression of c-Myc, CDK4 and E2F1, and the phosphorylation level of Rb protein, but upregulated p21 [3].

In mice transplanted with B16 murine melanoma, Oxamflatin (20 mg/kg) injected intraperitoneally six times on day 1, 3, 5, 7, 9 and 11 significantly increased the days of survival [1].

References:
Kim YB, Lee KH, Sugita K, et al.  Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase. Oncogene. 1999 Apr 15;18(15):2461-70.
Yin H, Zhang Y, Zhou X, et al.  Histonedeacetylase inhibitor Oxamflatin increase HIV-1 transcription by inducing histone modification in latently infected cells. Mol Biol Rep. 2011 Nov;38(8):5071-8.
Wang YL, Liui HL, Fu RG, et al.  HDAC Inhibitor Oxamflatin Induces Morphological Changes and has Strong Cytostatic Effects in Ovarian Cancer Cell Lines. Curr Mol Med. 2016;16(3):232-42.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt342.37
Cas No.151720-43-3
FormulaC17H14N2O4S
SolubilitySoluble in DMSO
Chemical Name(1Z,2E)-N-hydroxy-5-(3-(phenylsulfonamido)phenyl)pent-2-en-4-ynimidic acid
SDFDownload SDF
Canonical SMILESOC(/C([H])=C([H])/C#CC1=CC(NS(C2=CC=CC=C2)(=O)=O)=CC=C1)=N\O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

Oxamflatin