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.

Physicochemical Properties

Molecular Formula	C24H22N4O4
Molecular Weight	430.46
CAS #	3031536-71-4
PubChem CID	165413064
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	6
Heavy Atom Count	32
Complexity	647
Defined Atom Stereocenter Count	0
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)

Biological Activity

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.

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.