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ChemicalBook--->CAS DataBase List--->158093-65-3

158093-65-3

158093-65-3 Structure

158093-65-3 Structure
IdentificationBack Directory
[Name]

PU139
[CAS]

158093-65-3
[Synonyms]

PU139
[Molecular Formula]

C12H7FN2OS
[MOL File]

158093-65-3.mol
[Molecular Weight]

246.26
Chemical PropertiesBack 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 InformationBack 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.
[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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