EC Number   |
Inhibitors |
Structure |
|---|
    2.3.1.32 | anacardic acid |
- |
   |
| 2.3.1.32 | anacardic acid |
10 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 95% |
|
| 2.3.1.32 | curcumin |
25 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 75% |
|
| 2.3.1.32 | garcinol |
10 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 80% |
|
| 2.3.1.32 | isogarcinol |
10 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 70% |
|
| 2.3.1.32 | LTK14 |
20 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 70% |
|
| 2.3.1.32 | more |
no inhibition by cysteine, glutathione, ascorbic acid, Zn2+, Mn2+, Co2+, Ni2+, Fe3+ or acetate |
|
| 2.3.1.32 | more |
no inhibition of p300 by 5-methoxy-2-methyl-1,4-naphthoquinone (RTK2, alkyl substitution of hydroxyl group), 5-ethoxy-2-methyl-1,4-naphthoquinone (RTK3, alkyl substitution of hydroxyl group), 5-isopropoxy-2-methyl-1,4-naphthoquinone (RTK4, alkyl substitution of hydroxyl group), and 5-[2-(dimethylamino)-ethoxy]-2-methyl-1,4-naphthoquinone (RTK10, N,N-dimethylamine substitution of hydroxyl group), less than 10% inhibition with 6-methyl-5,8-dioxo-5,8-dihydronaphthalen-1-yl acetate (RTK5, acetyl substitution of hydroxyl group), 6-methyl-5,8-dioxo-5,8-dihydronaphthalen-1-yl methanesulfonate (RTK6, sulfonyl substitution of hydroxyl group), 2-methyl-5-(2-piperidin-1-ylethoxy)-1,4-naphthoquinone (RTK7, piperidine substitution of hydroxyl group), 2-methyl-5-(2-morpholin-4-ylethoxy)-1,4-naphthoquinone (RTK8, morpholine substitution of hydroxyl group), and ethyl [(6-methyl-5,8-dioxo-5,8-dihydronaphthalen-1-yl)-oxy]acetate (RTK9, ester substitution of hydroxyl group) |
|
| 2.3.1.32 | phosphate |
above 0.1 mM |
|
| 2.3.1.32 | Plumbagin |
RTK1, naturally occurring hydroxynaphthoquinone, isolated from Plumbago rosea roots, inhibits histone acetylation, and induces apoptosis at higher concentrations, it inhibits p300/CBP-mediated acetylation of p53 lysine 373 non-competitively, 25 microM inhibit histidine-tagged recombinant p300 with purified human HeLa core histone as substrate by about 60% compared to control; RTK1, naturally occurring hydroxynaphthoquinone, isolated from Plumbago rosea roots, it does not inhibit PCAF acetylation of p53 lysine 320 in vivo in HEK-293 cells (pretreated with acetylation inducer doxorubicin), but 10, 25, and 50 microM inhibit FLAG-tagged recombinant PCAF in vitro (30°C) with purified human HeLa core histone as substrate |
|
