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C646 is a selective inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. C646 preferentially selective for p300 versus other acetyltransferases.
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.
| Molecular Weight | 445.42 |
| Formula | C24H19N3O6 |
| CAS Number | 328968-36-1 |
| Solubility (25°C) | DMSO 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Fang Fang, et al. C646 modulates inflammatory response and antibacterial activity of macrophage
| Related Histone Acetyltransferase Products |
|---|
| CBP/p300-IN-5
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor, has an IC50 of 18.8 nM. |
| JG-2016
JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1), with an IC50 of 14.8 μM in the HAT1 acetylation assays. |
| AU-18069
AU-18069 is a CBP/p300 HAT inhibitor that can be used in studies related to hematological and solid tumors. |
| KAT modulator-1
KAT modulator-1 is a KAT modulator. |
| KAT6-IN-1
KAT6-IN-1 is a potent KAT6 inhibitor. |
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