PU139 manufacturers
- PU139
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- $48.00 / 1mg
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2026-04-20
- CAS:158093-65-3
- Min. Order:
- Purity: 99.96%
- Supply Ability: 10g
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| Product Name: | PU139 | | Synonyms: | PU139;Isothiazolo[5,4-b]pyridin-3(2H)-one, 2-(4-fluorophenyl)-;2-(4-Fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one | | CAS: | 158093-65-3 | | MF: | C12H7FN2OS | | MW: | 246.26 | | EINECS: | | | Product Categories: | API | | Mol File: | 158093-65-3.mol |  |
| | PU139 Chemical Properties |
| 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 |
| | PU139 Usage And Synthesis |
| 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 8mg/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 1h. | | 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) | | 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. |
| | PU139 Preparation Products And Raw materials |
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