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NiCur is an effective and selective inhibitor of CBP histone acetyltransferase (HAT), with an IC50 of 0.35 μM. NiCur blocks CBP HAT activity, downregulates p53 activation and inhibits apoptosis, while promoting methylation of Lysine 27 on histone H3, inhibiting Caspase 3 activity and PARP cleavage.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $43 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $148 | In Stock | |
25 mg | $286 | In Stock | |
50 mg | $425 | In Stock | |
100 mg | $619 | In Stock | |
200 mg | $873 | In Stock |
Description | NiCur is an effective and selective inhibitor of CBP histone acetyltransferase (HAT), with an IC50 of 0.35 μM. NiCur blocks CBP HAT activity, downregulates p53 activation and inhibits apoptosis, while promoting methylation of Lysine 27 on histone H3, inhibiting Caspase 3 activity and PARP cleavage. |
Targets&IC50 | CBP-HAT:0.35 μM |
In vitro | When NiCur acts on U2OS cells within the concentration range of 0.5 - 1 μM, it can reduce Dox-induced p53K382ac, p53S15p, and p53 levels in a dose-dependent manner [1]. At a concentration of 1.5 μM, NiCur can decrease H3K27ac levels; similarly, at 1.5 μM, NiCur can restore cell proliferation capacity. In intestinal epithelial cells, NiCur downregulates Dox-mediated p53 activation but does not affect H2A.X S139p levels. NiCur can modulate gene regulatory switches, thereby reprogramming the chromatin landscape, and can block CBP HAT activity [1]. |
Molecular Weight | 324.38 |
Formula | C22H16N2O |
Cas No. | 2674753-39-8 |
Smiles | C(=C\1/C(=O)\C(=C\C2=CC(C#N)=CC=C2)\CCC1)\C3=CC(C#N)=CC=C3 |
Color | Yellow |
Appearance | Solid |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (123.31 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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