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PRMT5:MEP50 PPI

Cat No.:V76608 Purity: ≥98%
PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor (antagonist) with anticancer effect and antiproliferation activity in lung and prostate cancer cells.
PRMT5:MEP50 PPI
PRMT5:MEP50 PPI Chemical Structure CAS No.: 3031536-71-4
Product category: Others 13
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Product Description
PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor (antagonist) with anticancer effect and antiproliferation activity in lung and prostate cancer cells.
Biological Activity I Assay Protocols (From Reference)
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].
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.
References

[1]. Discovery and Biological Characterization of PRMT5:MEP50 Protein-Protein Interaction Inhibitors. J Med Chem. 2022 Oct 7.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H22N4O4
Molecular Weight
430.46
CAS #
3031536-71-4
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO :~200 mg/mL (~464.62 mM)
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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