Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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CMP-5 (PRMT5-IN-5) is a first-in-class and specific PRMT5 inhibitor with anticancer (B-cell lymphomas) and immunomodulatory activity. It displays no activity against other type I (PRMT1 and PRMT4) and type II (PRMT7) enzymes. CMP-5 blocks EBV-driven B-lymphocyte transformation and survival, without effect on normal B cells. Inhibition of PRMT5 leads to lost recruitment of a PRMT5/p65/HDAC3-repressive complex on the miR96 promoter, restored miR96 expression, and PRMT5 downregulation.
ln Vitro |
Although CMP-5 (0-100 μM; 24-72 hours) exerts effects, even after prolonged times, its toxicity to normal resting B is limited [1]. In comparison to the group treated with DMSO, CMP-5 (40 μM; 24 hours) decreased the expression of p-BTK and pY (416) SRC in 60A cells [1]. PRMT5 is preferentially transcribed in Th1 cells as opposed to Th2 cells when exposed to CMP-5 (0–40 μM; 24 hours); in human Th1 cells and Th2 cells, the IC50 values are 26.9 μM and 31.6 μM, respectively. CMP-5 (25 μM; 24 hours) decreased mouse Th1 cell proliferation by 91%. Different IL-2 dosages were applied, and the maximum degree of IL-2-enhanced proliferation was seen at 5 ng/mL [1].
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Cell Assay |
Western Blot analysis [1]
Cell Types: 60A Cell Tested Concentrations: 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of p-BTK and pY(416)SRC protein levels. Cell viability assay [1] Cell Types: human Th1 cells and Th2 cells Tested Concentrations: 25 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited mouse Th1 cell proliferation, but adding IL-2 dose-dependently increased cell proliferation. |
References |
[1]. Alinari L, et al. Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation.Blood. 2015 Apr 16;125(16):2530-43.
[2]. Webb LM, et al. PRMT5-Selective Inhibitors Suppress Inflammatory T Cell Responses and Experimental Autoimmune Encephalomyelitis. J Immunol. 2017 Feb 15;198(4):1439-1451. |
Molecular Formula |
C₂₁H₂₁N₃
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Molecular Weight |
315.41
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CAS # |
880813-42-3
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Related CAS # |
CMP-5 hydrochloride;1030021-40-9
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SMILES |
N1(C([H])([H])C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C2C2C([H])=C(C([H])([H])N([H])C([H])([H])C3=C([H])C([H])=C([H])C([H])=N3)C([H])=C([H])C1=2
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Synonyms |
CMP5 CMP 5
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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 : ~125 mg/mL (~396.31 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (19.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 62.5 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. Solubility in Formulation 2: ≥ 6.25 mg/mL (19.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | |
5 mM | 0.6341 mL | 3.1705 mL | 6.3410 mL | |
10 mM | 0.3170 mL | 1.5852 mL | 3.1705 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.