Description |
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
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Target |
Ki: 400 nM (histone acetyltransferase p300)
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In Vitro |
C646 is a linear competitive inhibitor of p300 versus acetyl-CoA with a Ki of 400 nM. C646 shows a noncompetitive pattern of p300 inhibition versus H4-15 peptide substrate. C646 treatment reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 has a more potent effect on cell growth than Lys-CoA-Tat does[1]. C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells[2]. C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG[3].
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Cell Assay |
Cells are seeded in 6-well plates, incubated at 37°C for 4-10 h for attachment, and exposed (or not) to C646. After incubation for 2 h, the cells are subjected (or not) to IR and incubated for 10 days for colony formation. The cells are fixed with methanol and stained with crystal violet. Colonies of at least 50 cells are counted. The surviving fraction is normalized to the corresponding controls. The dose required to reduce the surviving fraction to 10% (D10) of the irradiated cells is calculated by using the linear-quadratic model.
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Density | 1.4±0.1 g/cm3 |
Boiling Point | 662.6±65.0 °C at 760 mmHg |
Flash Point | 354.5±34.3 °C |
Exact Mass | 445.127380 |
PSA | 128.93000 |
LogP | 4.87 |
Vapour Pressure | 0.0±2.1 mmHg at 25°C |
Storage condition | 2-8°C |