PU139 |
| Catalog No.GC63405 |
Le PU139 est un puissant inhibiteur pan-histone de l'acétyltransférase (HAT). PU139 bloque les HAT Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) et p300 avec des IC50 de 8,39, 9,74, 2,49 et 5,35 μM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 158093-65-3
Sample solution is provided at 25 µL, 10mM.
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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[1][2].
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)[1].PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH[1].
PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition[1].
[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.
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