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.
性状
Solid
IC50 & Target[1][2]
GCN5 8.39 μM (IC50) CREBBP 2.49 μM (IC
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male NMRI:nu/nu mic
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Gajer JM, et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis. 2015;4(2):e137. Published 2015 Feb 9. [2]. Carneiro VC, et al. Epigenetic changes modulate schistosome egg formation and are a novel target for reducing transmission of schistosomiasis. PLoS Pathog. 2014;10(5):e1004116. Published 2014 May 8.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (50.76 mM; ultrasonic and warming and heat to 60°C)配制储备液