PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC 50 s of 8.39, 9.74, 2.49 and 5.35 μM, respectively In Vitro PU139 inhibits cell growth with GI 50 s of In Vivo PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male NMRI:nu/nu mice (Neuroblastoma xenografts) Dosage: 25 mg/kg Administration: Intraperitoneally (PU139) with Dxorubicin at 8 mg/kg i.v.; Administered on days 14 and 21 as a single dose of each compound or, for combination therapy; both drugs were administered successively within 1 h. Result: Optimum growth inhibition following a single PU139 therapy was moderate, but significant as compared with the untreated group and confirmed the previous findings. Form:Solid IC50& Target:GCN5 8.39 μM (IC 50 ) CREBBP 2.49 μM (IC 50 ) PCAF 9.74 μM (IC 50 ) p300 5.35 μM (IC 50 )
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PU139
CAS number:158093-65-3 molecular formula:C12H7FN2OS
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 158093-65-3 | molecular formula | C12H7FN2OS |
| molecular weight | 246.26 g/mol | Exact mass | ≥98% |
| PSA | 58.500 Ų | logp | 2.400 |
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