| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
PU139's primary targets are histone acetyltransferases (HATs), specifically Gcn5, p300/CBP-associated factor (PCAF), CREB-binding protein (CBP), and p300. It blocks the activity of these enzymes with IC50 values of 8.39 μM for Gcn5, 9.74 μM for PCAF, 2.49 μM for CBP, and 5.35 μM for p300, respectively.
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| ln Vitro |
With GI50 <60 μM, PU139 suppresses the growth of A431, A549, A2780, HepG2, SW480, U-87MG, HCT116, SK-N-SH, and MCF7 cells [1]. In SK-N-SH neuroblastoma cell line, PU139 (0-100 μM; 24-72 hours) causes caspase-independent cell death [1].
In vitro, PU139 acts as a pan-HAT inhibitor, effectively blocking the enzymatic activity of multiple HATs. Its inhibitory activity is characterized by its IC50 values against its target enzymes, demonstrating its potency in cell-free systems. |
| ln Vivo |
PU139 (25 mg/kg; intraperitoneal injection) has a synergistic effect in growth inhibition with doxorubicin, which is used as a prototype chemotherapeutic agent [1].
Specific in vivo activity data for PU139 is not detailed in the provided search results. As a research tool for epigenetic studies, its primary application is in in vitro and cell-based assays to elucidate the function of HATs. |
| Enzyme Assay |
The in vitro activity of PU139 is typically assessed using cell-free HAT enzyme activity assays. In these assays, the specific HAT enzyme (e.g., p300, CBP, PCAF, or Gcn5) is incubated with a histone substrate and acetyl-CoA in the presence of varying concentrations of PU139. The incorporation of acetyl groups into the histone substrate is measured, often using radioactive or fluorescence-based detection methods, to determine the IC50.
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| Cell Assay |
For cellular assays, various cancer cell lines are treated with PU139 to assess its effects on histone acetylation and cell proliferation. Cells are cultured in appropriate media and exposed to different concentrations of PU139 for specified periods. The levels of histone acetylation are then analyzed by Western blotting using acetylation-specific antibodies. Cell viability and proliferation are assessed using standard assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
Animal/Disease Models: Male NMRI: nu/nu (nude) mice (neuroblastoma xenograft) [1]
Doses: 25 mg/kg Route of Administration: Adriamycin 8 mg/kg iv intraperitoneally (ip) (ip) (PU139); at p. 14 Days 1 and 21 are administered as a single dose of each compound, or for combination treatment; both drugs are administered sequentially within 1 hour. Experimental Results: Optimal growth inhibition after single PU139 treatment was moderate but significant compared with the untreated group and confirmed previous findings. In vivo studies for PU139 are not described in the provided search results. As a research compound, its effects are primarily studied in vitro and in cellular models to investigate the biological roles of HATs. |
| ADME/Pharmacokinetics |
PU139 has a molecular weight of 246.26 g/mol and a molecular formula of C12H7FN2OS. It is soluble in DMSO at 10 mg/mL with ultrasonic and warming assistance. The compound has a calculated XLogP3-AA value of 2.4. It should be stored at 4°C in a dry, sealed container.
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| Toxicity/Toxicokinetics |
Specific toxicity data for PU139 is not available in the provided search results. As a research chemical, standard laboratory safety precautions should be followed when handling the compound. Its safety profile has not been fully established for therapeutic use.
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| References |
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| Additional Infomation |
PU139 is a research compound used to study the role of histone acetyltransferases in epigenetic regulation and gene expression. It serves as a valuable tool for investigating the potential of HAT inhibitors in various diseases, including cancer. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C12H7FN2OS
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| Molecular Weight |
246.2594
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| Exact Mass |
246.026
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| CAS # |
158093-65-3
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| Related CAS # |
158093-65-3;
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| PubChem CID |
9992116
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
434.3±51.0 °C at 760 mmHg
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| Flash Point |
216.5±30.4 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.686
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| LogP |
1.83
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(N=C1)SN(C2=O)C3=CC=C(C=C3)F
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| InChi Key |
QMCIVCACYJRAAY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H7FN2OS/c13-8-3-5-9(6-4-8)15-12(16)10-2-1-7-14-11(10)17-15/h1-7H
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| Chemical Name |
2-(4-Fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
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| Synonyms |
PU139 PU-139 PU 139
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~40.61 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0607 mL | 20.3037 mL | 40.6075 mL | |
| 5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL | |
| 10 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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