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 IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
体外研究
PU139 inhibits cell growth with GI50s of <60 μM (A431, A549, A2780, HepG2, SW480, U-87 MG, HCT116 and SK-N-SH and MCF7 cells).
PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH.
体内研究
PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition.
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.
分子式
C12H7FN2Os
分子量
246.26
CAS号
158093-65-3
运输条件
Room temperature in continental US; may vary elsewhere.