| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PRMT5:MEP50 PPI targets the protein-protein interaction between PRMT5 and MEP50. By inhibiting the formation of this complex, it blocks the methyltransferase activity of PRMT5, which normally catalyzes the symmetric dimethylation of arginine residues in target proteins, including histones. This disruption of the PRMT5:MEP50 PPI is a therapeutic strategy for cancers.
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| ln Vitro |
Prostate cancer cell proliferation is inhibited by PRMT5:MEP50 PPI (0–10 μM; 72 h)[1]. In prostate cancer cells, PRMT5:MEP50 PPI (250-1000 nM; 72 h) reduces the expression of the global arginine 3 residue of histone H4 (H4R3me2s) level[1]. Prostate cancer cells' PRMT5:MEP50-regulated IVL gene is de-repressed by PRMT5:MEP50 PPI (500 nM; 72 h)[1]. Treatment with PRMT5:MEP50 PPI affects several PRMT5-regulated pathways that are essential to the survival and growth of cancer cells in the prostate and lung[1].
In vitro, PRMT5:MEP50 PPI (0-10 microM; 72 hours) inhibits prostate cancer cell proliferation (LNCaP cells) with an IC50 value of 430.2 nM. At 500 nM for 72 hours, it relieves PRMT5:MEP50-mediated repression of the IVL gene. At 250-1000 nM, it decreases global H4R3me2s levels by 65%. It also inhibits PRMT5-regulated pathways critical for cancer cell survival. |
| ln Vivo |
In vivo, PRMT5:MEP50 PPI shows anti-tumor activity. By inhibiting the PRMT5:MEP50 protein-protein interaction, it disrupts key epigenetic and signaling pathways. This inhibition leads to reduced cell proliferation and tumor growth in models of lung and prostate cancer. It is a potent PPI inhibitor with a molecular weight of 430.46 g/mol.
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| Enzyme Assay |
A cell-free binding assay for PRMT5:MEP50 PPI would involve SPR or TR-FRET. Recombinant PRMT5 and MEP50 proteins are used. The compound is tested for its ability to disrupt the interaction between purified PRMT5 and MEP50. A biochemical methylation assay using a histone H4 peptide substrate can also measure the inhibition of PRMT5 methyltransferase activity.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: LNCaP cells Tested Concentrations: 0-10 μM Incubation Duration: 72 h Experimental Results: demonstrated IC50 value of 430.2 nM. Western Blot Analysis[1] Cell Types: LNCaP cells Tested Concentrations: 250, 500 and 1000 nM Incubation Duration: 72 h Experimental Results: Observed global arginine 3 residue of histone H4(H4R3me2s) diminished by 65%. RT-PCR[1] Cell Types: LNCaP cells Tested Concentrations: 500 nM Incubation Duration: 72 h Experimental Results: De-repressed the PRMT5: MEP50-regulated IVL gene without Dramatically altering the expression of the PRMT5: pICln-regulated AR gene. LNCaP prostate cancer cells are seeded in 96-well plates (5,000 cells/well) in RPMI-1640 + 10% FBS. After 24 hours, cells are treated with PRMT5:MEP50 PPI (0-10 uM) for 72 hours. Cell viability is measured using the MTT or CellTiter-Glo assay to determine the IC50 (430.2 nM). For Western blot, cells are treated with 250-1000 nM for 72 hours, and H4R3me2s levels are assessed. |
| Animal Protocol |
A standard in vivo animal protocol for PRMT5:MEP50 PPI would involve mouse xenograft models. Female BALB/c nude mice are implanted subcutaneously with LNCaP or A549 cells. When tumors reach 100-150 mm3, mice are randomized and treated intraperitoneally with the PPI inhibitor (10-50 mg/kg). Tumor volume and body weight are measured. H4R3me2s levels in tumor lysates are measured by Western blot.
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| ADME/Pharmacokinetics |
PRMT5:MEP50 PPI has a molecular weight of 430.46 and the molecular formula C24H22N4O4. The product is a solid powder that should be stored at -20degC for up to 3 years. In solution, it is stable for 6 months at -80degC. It is soluble in DMSO (>200 mg/mL). For in vivo use, it can be formulated in 10% DMSO/PEG/Tween-80/saline.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PRMT5:MEP50 PPI are not available. As a research chemical, standard laboratory safety precautions should be followed. Its safety profile has not been established for clinical use. The compound is handled as a potent biological research tool in laboratory settings.
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| References | |
| Additional Infomation |
PRMT5:MEP50 PPI (CAS: 3031536-71-4) is a research-grade chemical and is not approved for clinical use. It is a novel PRMT5:MEP50 protein-protein interaction inhibitor that shows anti-tumor and anti-proliferative activity against lung and prostate cancer cells. It is a valuable research tool for studying PRMT5 biology and for validating this PPI as a therapeutic target.
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| Molecular Formula |
C24H22N4O4
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| Molecular Weight |
430.46
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| Exact Mass |
430.164
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| CAS # |
3031536-71-4
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| PubChem CID |
165413064
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
647
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=NOC(=C1COC2=CC=CC(=C2)C(=O)NNC(=O)C3=NC4=CC=CC=C4C=C3)C
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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 :~200 mg/mL (~464.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3231 mL | 11.6155 mL | 23.2310 mL | |
| 5 mM | 0.4646 mL | 2.3231 mL | 4.6462 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3231 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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