Network Version
C646 Data Sheet
| Product Name: | C646 |
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|---|---|---|
| CAS No.: | 328968-36-1 | |
| Cat. No.: | HY-13823 | |
| MWt: | 445.42 | |
| Formula: | C24H19N3O6 | |
| Purity : | >98% | |
| Solubility: | DMSO : 16.67 mg/mL (37.43 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1]. IC50 & Target: Ki: 400 nM (histone acetyltransferase p300) 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]. 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[4]. | ||
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