PU139 |
| カタログ番号GC63405 |
PU139 は、強力な汎ヒストン アセチルトランスフェラーゼ (HAT) 阻害剤です。 PU139 は、HAT の Gcn5、p300/CBP 関連因子 (PCAF)、CREB (cAMP 応答要素結合) タンパク質 (CBP)、および p300 をそれぞれ 8.39、9.74、2.49、および 5.35 μM の IC50 でブロックします。
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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