| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
MRE11
MRE11 endonuclease (component of MRN complex). |
|---|---|
| ln Vitro |
PFM01 significantly lessens the double-strand break (DSB) repair defect caused by mirin or PFM39 in irradiated G2 cells.It also rescues the repair defect in 48BR (WT) and HSC62 (BRCA2-defective) primary cells, diminishes the formation of RAD51 foci in 1BR3 (WT) and HSC62 (BRCA2-defective) cells, enhances non-homologous end-joining (NHEJ) in H1299 dA3 cells, and decreases homologous recombination (HR) in U2OS DR-GFP cells.[1]
PFM01 selectively inhibits MRE11 endonuclease activity. By targeting MRE11 at a site close to the dimer interface, it disrupts the ssDNA-binding groove. It significantly lessens the double-strand break (DSB) repair defect caused by mirin or PFM39 in irradiated G2 cells. It rescues repair defects in 48BR (WT) and HSC62 (BRCA2-defective) primary cells. It diminishes RAD51 foci formation, enhances NHEJ, and decreases HR. |
| ln Vivo |
In vivo, PFM01 has been shown to regulate double-strand break repair by promoting NHEJ and reducing HR. It has been studied in mouse models to evaluate its effects on DNA repair and sensitivity to DNA-damaging agents. By inhibiting MRE11 endonuclease, it can modulate the DNA damage response and potentially sensitize tumors to radiation or chemotherapy.
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| Enzyme Assay |
PFM01 is evaluated in cell-free nuclease assays using purified MRE11 protein. The compound is incubated with MRE11 and a DNA substrate containing a double-strand break, and the inhibition of endonuclease activity is measured. Endonuclease activity is assessed by detecting DNA cleavage products using gel electrophoresis or fluorescence-based methods.
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| Cell Assay |
The following fibroblast types were cultured in Dulbecco's modified Eagles medium: 48BR (human primary fibroblasts), ATLD2 (primary fibroblasts), 1BR3 hTERT, HSC62 hTERT (BRCA2-defective), and 2BN hTERT (XLF-defective) (12%). In minimal essential medium (MEM) supplemented with 10% FCS, A549 cells were cultivated. The medium was exposed to 137Cs radiation on the cells. The concentrations of MRE11 inhibitors were, unless specified otherwise, 500 μM Mirin, 100 μM PFM39, 100 μM PFM01, and 100 μM PFM03. 30 minutes before irradiation, either 10 μM ATM inhibitor (KU55933) or 10 μM DNA-PKcs inhibitor (NU7441) were added, unless otherwise specified.
PFM01 is assessed in cell-based assays using fibroblast cell lines (e.g., 48BR, HSC62, 1BR3, H1299, U2OS). Cells are treated with PFM01 (typically 100 μM), and DNA repair is assessed by measuring the formation of RAD51 foci (HR) or NHEJ efficiency. Cell viability and sensitivity to radiation or DNA-damaging agents may also be evaluated. |
| Animal Protocol |
PFM01 is administered in animal models to evaluate its effects on DNA repair and tumor sensitivity to therapy. Efficacy is assessed in tumor xenograft models, where tumor growth inhibition in combination with radiation or chemotherapy is measured. Pharmacokinetic studies are conducted to assess bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
No detailed PK data available. PFM01 has a molecular weight of 293.40. Soluble in DMSO. Purity ≥98%.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only, not for human use.
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| References | |
| Additional Infomation |
PFM01 is a selective MRE11 endonuclease inhibitor. Molecular formula: C14H15NO2S2; MW: 293.40. Cell-permeable N-alkylated Mirin derivative. Enhances NHEJ and reduces HR. For research use only.
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| Molecular Formula |
C14H15NO2S2
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|---|---|
| Molecular Weight |
293.399
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| Exact Mass |
293.054
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| Elemental Analysis |
C, 57.31; H, 5.15; N, 4.77; O, 10.91; S, 21.85
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| CAS # |
1558598-41-6
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| Related CAS # |
1558598-41-6
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| PubChem CID |
2145809
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
435.2±55.0 °C at 760 mmHg
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| Flash Point |
217.0±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
2.74
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
398
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1/C(=C\C2=CC=C(O)C=C2)/C(=O)N(CC(C)C)C1=S
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| InChi Key |
GPURHDUTZUYAFI-GHXNOFRVSA-N
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| InChi Code |
InChI=1S/C14H15NO2S2/c1-9(2)8-15-13(17)12(19-14(15)18)7-10-3-5-11(16)6-4-10/h3-7,9,16H,8H2,1-2H3/b12-7-
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| Chemical Name |
(5Z)-5-[(4-hydroxyphenyl)methylidene]-3-(2-methylpropyl)-2-sulfanylidene-1,3-thiazolidin-4-one
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| Synonyms |
PFM01; PFM-01; PFM 01
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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 |
| 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: ≥ 100 mg/mL (~340.8 mM)
Ethanol: ~25 mg/mL (~85.2 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 | 3.4083 mL | 17.0416 mL | 34.0832 mL | |
| 5 mM | 0.6817 mL | 3.4083 mL | 6.8166 mL | |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4083 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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