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NiCur

Catalog No. T60888

NiCur blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC 50 value of 0.35 μΜ. NiCur can be used to perform mechanistic studies without affecting target proteins expression [1].

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NiCur Chemical Structure
NiCur, CAS N/A
Pack Size Availability Price/USD Quantity
100 mg 10-14 weeks $ 1,190.00
200 mg 10-14 weeks $ 1,842.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
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Description NiCur blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC 50 value of 0.35 μΜ. NiCur can be used to perform mechanistic studies without affecting target proteins expression [1].
In vitro In U2OS cells, NiCur applied at concentrations of 0.5 to 1 μM significantly diminishes Dox-induced acetylation at lysine 382 on p53 (p53K382ac), phosphorylation at serine 15 on p53 (p53S15p), and overall p53 levels in a dose-dependent fashion. At a higher concentration of 1.5 μM, NiCur lowers acetylation at lysine 27 on histone H3 (H3K27ac) and restores cell proliferation in these cells. Moreover, in intestinal epithelial cells, NiCur suppresses Dox-induced activation of p53 without altering acetylation at serine 139 on histone H2A.X (H2A.X S139p). NiCur thus serves as a modulator of gene regulation by reprogramming the chromatin landscape, primarily by inhibiting CBP histone acetyltransferase (HAT) activity. Western Blot Analysis in U2OS cells corroborates these findings, showing a concentration-dependent reduction in p53K382ac, p53S15p, and p53 levels with NiCur treatment.
Molecular Weight 324.38
Formula C22H16N2O

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

NiCur inhibitor inhibit

 

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