PU-139

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PU-139 是一种有效的、非选择性的 HAT（组蛋白乙酰转移酶）抑制剂。

PU-139 is a potent, unselective HAT (Histone acetyltransferase) inhibitor that blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB protein (CBP) and p300; triggers caspase-independent cell death in cell culture, blocks growth of SK-N-SH neuroblastoma xenografts in mice, and synergizes the effect of doxorubicin in vivo.

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.

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.

PU139 | PU 139

Chromatin/Epigenetic

HAT

HAT

——

——

158093-65-3

246.259

C12H7FN2OS

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (40.61 mM)

O=C1N(C2=CC=C(F)C=C2)SC3=NC=CC=C31

2-(4-fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one

(-20℃)

With Ice Pack

≥ 2 years