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C646
CAS No. : 328968-36-1
MCE 国际站：C646
产品活性：C646 是一种竞争性的选择性 histone acetyltransferase p300 抑制剂，Ki 值为 400 nM，对其他的乙酰转移酶作用较小。
研究领域：Epigenetics | Autophagy | Apoptosis
作用靶点：Histone Acetyltransferase | Autophagy | Epigenetic Reader Domain | Apoptosis
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 the 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. C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells. C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG.
In Vivo: Suppression of P300 by c646 (intraperitoneally injected, 30 nmol/g/d for 2 weeks) dramatically reduces the level of blood glucose in db/db mice.
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