PU139 is a strong inhibitor of pan-histone acetyltransferase (HAT). It effectively inhibits the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP), and p300 with IC50 values of 8.39, 9.74, 2.49, and 5.35 μM, respectively [1][2].
体内研究
PU139 (25 mg/kg; i.p.) enhances the growth inhibition of Doxorubicin, a prototypic chemotherapeutic drug [1].
体外研究
PU139 suppresses cell growth with GI50 values below 60 μM in A431, A549, A2780, HepG2, SW480, U-87, MG, HCT116, SK-N-SH, and MCF7 cells [1].
PU139 (0-100 μM; 24-72 hours) induces caspase-independent cell death in the neuroblastoma cell line SK-N-SH [1].
PU139 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293 cells
2 µM
24 hours
To evaluate the effect of PU139 on Smp14 promoter activity. PU139 significantly inhibited the SmCBP1- and SmGCN5-mediated transcriptional activity of the Smp14 promoter.
PLoS Pathog. 2014 May 8;10(5):e1004116
HCT116 colon carcinoma cells
25 µM
3 hours
Evaluate the effect of HAT inhibitors on histone acetylation levels, results showed PU139 decreased SAHA-induced H3K14 and H4K8 hyperacetylation.
Oncogenesis. 2015 Feb 9;4(2):e137
SK-N-SH neuroblastoma cells
25 µM
3 hours
Evaluate the effect of HAT inhibitors on histone acetylation levels, results showed PU139 decreased SAHA-induced H3K14 and H4K8 hyperacetylation.
Oncogenesis. 2015 Feb 9;4(2):e137
PU139 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Schistosoma mansoni
Adult worm pairs
In vitro culture
20 µM
Medium refreshed every 24 hours for 2-4 days
To evaluate the effect of PU139 on Smp14 expression and egg development. PU139 significantly reduced Smp14 mRNA and protein levels, leading to abnormal egg morphology and defective eggshells.
PLoS Pathog. 2014 May 8;10(5):e1004116
NMRI:nu/nu mice
SK-N-SH neuroblastoma xenograft model
Intraperitoneal injection
25 mg/kg
Once per week for 24 days
Evaluate the antitumor effect of PU139, results showed PU139 significantly reduced tumor volume (33%).
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