| Chemical Properties | Back Directory | [Boiling point ]
434.3±51.0 °C(Predicted) | [density ]
1.473±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture | [solubility ]
DMSO : 12.5 mg/mL (50.76 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
0.43±0.20(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [in vivo]
PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition[1]. | Animal Model: | Male NMRI:nu/nu mice (Neuroblastoma xenografts)[1] | | 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.
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| [IC 50]
GCN5: 8.39 μM (IC50); CREBBP: 2.49 μM (IC50); PCAF: 9.74 μM (IC50); p300: 5.35 μM (IC50) | [storage]
4°C, away from moisture | [References]
[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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