C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
体外研究
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. 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.
体内研究
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.
Animal Model:
Fourteen-week-old male db/db mice and normal m/m mice
Dosage:
30 nmol/g
Administration:
Intraperitoneally injected; daily; 2 weeks
Result:
The db/db mice showed greater body masses and higher levels of fasting blood glucose than the m/m mice.
分子式
C20H22N3O3S2Cl
分子量
445.42
CAS号
328968-36-1
运输条件
Room temperature in continental US; may vary elsewhere.