PU139
Based on 4 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 158093-65-3
- Formula: C12H7FN2OS
- Molecular Weight:246.26
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Obesity Compound Library
HY-L087
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Anti-Pulmonary Fibrosis Compound Library
HY-L125
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Pain-Related Compound Library
HY-L139
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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Epigenetics Compound Library Mini
HY-L005M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) PU139
More
Biological Activity
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GCN5 8.39 μM (IC50) |
CREBBP 2.49 μM (IC50) |
PCAF 9.74 μM (IC50) |
p300 5.35 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | GI50 |
3.42 μM
Compound: 1, PU139
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Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
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10.1039/C4MD00245H |
| HL-60 | GI50 |
3.42 μM
Compound: 67
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Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
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[PMID: 33045661] |
| LNCaP | GI50 |
36.2 μM
Compound: 1, PU139
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Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
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10.1039/C4MD00245H |
| MCF7 | GI50 |
37.2 μM
Compound: 4d
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Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
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[PMID: 21353783] |
| Sf9 | IC50 |
10 μM
Compound: PU139
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Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after
Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after
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[PMID: 31910017] |
| SK-N-SH | GI50 |
10.3 μM
Compound: 4d
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Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
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[PMID: 21353783] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI:nu/nu mice (Neuroblastoma xenografts)[1]
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Dosage:25 mg/kg
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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.
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Result:Optimum growth inhibition following a single PU139 therapy was moderate, but significant as compared with the untreated group and confirmed the previous findings.
Chemical Information
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CAS No. 158093-65-3
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Appearance Solid
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Molecular Weight 246.26
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Formula C12H7FN2OS
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Color Off-white to yellow
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SMILES
O=C1N(C2=CC=C(F)C=C2)SC3=NC=CC=C31
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Tumor cells impair immunological synapse formation via central nervous system-enriched metabolite. [Abstract]2024 Jun 10;42(6):985-1002.e18. PMID: 38821061 -
Ecotoxicol Environ Saf
Nicotine interacts with DNA lesions induced by alpha radiation which may contribute to erroneous repair in human lung epithelial cells. [Abstract]2024 Sep 7:284:117009. PMID: 39244876 -
Plant J
Sexually dimorphic acetyl-CoA biosynthesis and utilization in response to drought and exogenous acetic acid. [Abstract]2024 Aug;119(4):1967-1985. PMID: 38944754 -
Solvent & Solubility
DMSO : 10 mg/mL (40.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (4.06 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Gajer JM, et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis. 2015;4(2):e137. Published 2015 Feb 9. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0607 mL | 20.3037 mL | 40.6075 mL | 101.5187 mL |
| 5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL | 20.3037 mL | |
| 10 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL | 10.1519 mL | |
| 15 mM | 0.2707 mL | 1.3536 mL | 2.7072 mL | 6.7679 mL | |
| 20 mM | 0.2030 mL | 1.0152 mL | 2.0304 mL | 5.0759 mL | |
| 25 mM | 0.1624 mL | 0.8121 mL | 1.6243 mL | 4.0607 mL | |
| 30 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3840 mL | |
| 40 mM | 0.1015 mL | 0.5076 mL | 1.0152 mL | 2.5380 mL |
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