| biological activity | L002 is a potent, cell-permeable, A reversible and specific acetyltransferase p300(KAT3B) inhibitor with an IC50 of 1.98 μm. L002 binds to the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential to be used in the study of cardiac hypertrophy and fibrosis caused by hypertension. |
| Target | IC50: 1.98 uM (KAT3B); 35 µm (PCAF); 34 µm (GCN5) ;STAT3; p53 |
|
Animal Model:
| Wild‐type C57BL/6 male mice planted with osmotic minipumps ( Angiotensin II 1500ng/kg/min) for 4 weeks |
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Dosage:
| 20μg/gm body weight; every 3rd day; 2 weeks |
|
Administration:
| Intraperitoneal injection |
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Result:
| Reversed hypertension-induced cardiac fibrosis in mice. |
