MS023
Based on 24 publication(s) in Google Scholar
MS023, a chemical probe, is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1831110-54-3
- Formula: C17H25N3O
- Molecular Weight:287.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
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Publications Citing Use of MedChemExpress (MCE) MS023
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
- Nat Commun. 2025 Jan 2;16(1):87. [Abstract]
- Nucleic Acids Res. 2026 Jun 22;54(12):gkag655. [Abstract]
- Acta Pharm Sin B. 2022 Apr;12(4):1840-1855. [Abstract]
- Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
- Sci Adv. 2026 Jan 23;12(4):eaea3960. [Abstract]
- Cell Commun Signal. 2025 Mar 8;23(1):126. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Int J Biol Macromol. 2024 Aug 1:134411. [Abstract]
- Cell Rep. 2024 Jul 24;43(8):114537. [Abstract]
- Cell Rep. 2021 Sep 21;36(12):109731. [Abstract]
- J Med Chem. 2025 Feb 27;68(4):4373-4381. [Abstract]
- Eur J Med Chem. 2025 Dec 15:300:118123. [Abstract]
- Cell Mol Life Sci. 2025 Apr 7;82(1):142. [Abstract]
- EMBO Rep. 2025 Oct 20. [Abstract]
- EMBO Rep. 2025 Oct 6. [Abstract]
- Oncogenesis. 2022 Aug 8;11(1):45. [Abstract]
- Cancer. 2024 Apr 15;130(S8):1415-1423. [Abstract]
- Neurochem Int. 2024 Jun:176:105728. [Abstract]
- Bone. 2023 Nov:176:116887. [Abstract]
- J Proteome Res. 2024 Mar 1;23(3):1014-1027. [Abstract]
- PLoS One. 2023 Dec 22;18(12):e0296291. [Abstract]
- bioRxiv. 2026 May 29.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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Cell Imaging/Staining
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IP
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WB
All Histone Methyltransferase Isoforms
More
Biological Activity
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PRMT1 |
PRMT3 |
PRMT6 |
PRMT8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
13.4 μM
Compound: Chemical probe: MS023
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Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
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[PMID: 33691794] |
| A549 | IC50 |
5.1 μM
Compound: Chemical probe: MS023
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Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)
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[PMID: 33691794] |
| HCC4006 | IC50 |
0.47 μM
Compound: Chemical probe: MS023
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Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
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[PMID: 33691794] |
| HCC4006 | IC50 |
0.56 μM
Compound: Chemical probe: MS023
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Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)
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[PMID: 33691794] |
| SK-LU-1 | IC50 |
36.7 μM
Compound: Chemical probe: MS023
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Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
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[PMID: 33691794] |
| SK-LU-1 | IC50 |
41 μM
Compound: Chemical probe: MS023
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Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)
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[PMID: 33691794] |
MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells[1].
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 and HEK293 cells
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Concentration:1.4, 4, 12, 37, 111, 333, and 1000 nM
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Incubation Time:48 hours for MCF7 cells; 20 hours for HEK293 cells
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Result:Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC50=9±0.2 nM).
Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56±7 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells[2]
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Dosage:160 mg/kg
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Administration:Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
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Result:Combinatorial treatment extended survival of leukemic mice relative to single treatments.
Chemical Information
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CAS No. 1831110-54-3
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Appearance Solid
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Molecular Weight 287.40
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Formula C17H25N3O
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Color White to light yellow
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SMILES
CN(CCN)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2025 Jan 22;16(1):949. PMID: 39843447
MS023 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
Representative images of FRAP of MSX1-mEGFP- expressing HEK293T treated with DMSO or MS023.
MS023 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
Representative western blot images of Co-IP assays assessing the aDMA of MSX1 in treated with MS023 or PRMT1 siRNA.
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Nat Commun
Positive feedback between arginine methylation of YAP and methionine transporter SLC43A2 drives anticancer drug resistance. [Abstract]2025 Jan 2;16(1):87. PMID: 39747898 -
Nucleic Acids Res
RECQ4 arginine methylation suppresses single-stranded DNA gap accumulation at replication forks. [Abstract]2026 Jun 22;54(12):gkag655. PMID: 42363758 -
Acta Pharm Sin B
2022 Apr;12(4):1840-1855. PMID: 35847488 -
Cell Rep Med
2026 Jan 20;7(1):102542. PMID: 41564858
MS023 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
The drug response curve and IC50 value for PRMT inhibitor MS023 and GSK591 combinations after U2AF2 knockdown in THP1 leukemia cells. Cell viability was assessed using a CCK8 assay.
MS023 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
RT-PCR results detecting aberrantly spliced transcripts in THP1 leukemia cells, which were treated with PRMT inhibitor MS023 or GSK591 with or without U2AF2 knockdown.
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Sci Adv
TDRD3, a Tudor domain-containing protein, regulates Klf2-dependent Treg differentiation and function to modulate immune tolerance. [Abstract]2026 Jan 23;12(4):eaea3960. PMID: 41576154 -
Cell Commun Signal
2025 Mar 8;23(1):126. PMID: 40057764
MS023 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Mar 8;23(1):126. [Abstract]
Immunoprecipitation and western blot analysis of arginine dimethylation in METTL14 overexpressed in HEK293T cells. Cells were treated with 1 μM EPZ015666, 1 μM MS023, or DMSO for 72 h and METTL14 is immunoprecipitated by anti-METTL14 antibody.
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Int J Biol Macromol
PRMT1 and TDRD3 promote stress granule assembly by rebuilding the protein-RNA interaction network. [Abstract]2024 Aug 1:134411. PMID: 39097054 -
Cell Rep
Arginine methylation-enabled FUS phase separation with SMN contributes to neuronal granule formation. [Abstract]2024 Jul 24;43(8):114537. PMID: 39052476 -
Cell Rep
The protein arginine methyltransferase PRMT1 promotes TBK1 activation through asymmetric arginine methylation. [Abstract]2021 Sep 21;36(12):109731. PMID: 34551290 -
J Med Chem
Opto-Epigenetic Regulation of Histone Arginine Asymmetric Dimethylation via Type I Protein Arginine Methyltransferase Inhibition. [Abstract]2025 Feb 27;68(4):4373-4381. PMID: 39961800 -
Eur J Med Chem
Discovery of novel indazole derivatives as type Ⅰ PRMTs inhibitors for the treatment of triple-negative breast cancer. [Abstract]2025 Dec 15:300:118123. PMID: 40929806 -
Cell Mol Life Sci
Dietary advanced glycation end-products exacerbate sarcopenia onset by activating apoptosis through PRMT1-mediated CRTC3 arginine methylation. [Abstract]2025 Apr 7;82(1):142. PMID: 40192801 -
EMBO Rep
Tudor-based proteomic strategy pan-specifically enriches and identifies protein arginine methylation. [Abstract]2025 Oct 20. PMID: 41116072 -
EMBO Rep
2025 Oct 6. PMID: 41053315 -
Oncogenesis
Methylation of HBP1 by PRMT1 promotes tumor progression by regulating actin cytoskeleton remodeling. [Abstract]2022 Aug 8;11(1):45. PMID: 35941115 -
Cancer
Type-I protein arginine methyltransferase inhibition primes anti-programmed cell death protein 1 immunotherapy in triple-negative breast cancer. [Abstract]2024 Apr 15;130(S8):1415-1423. PMID: 38079306 -
Neurochem Int
The antidepressant effects of protein arginine methyltransferase 2 involve neuroinflammation. [Abstract]2024 Jun:176:105728. PMID: 38561150 -
Bone
PRMT1-mediated arginine methylation promotes postnatal calvaria bone formation through BMP-Smad signaling. [Abstract]2023 Nov:176:116887. PMID: 37634683 -
J Proteome Res
ETD-Based Proteomic Profiling Improves Arginine Methylation Identification and Reveals Novel PRMT5 Substrates. [Abstract]2024 Mar 1;23(3):1014-1027. PMID: 38272855 -
PLoS One
Asymmetric and symmetric protein arginine methylation in methionine-addicted human cancer cells. [Abstract]2023 Dec 22;18(12):e0296291. PMID: 38134182 -
Solvent & Solubility
DMSO : 100 mg/mL (347.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Saline
Solubility: 53.33 mg/mL (185.56 mM); Clear solution; Need ultrasonic and adjust pH to 8 with 1M HCl
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81. [Content Brief]
[2]. Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4795 mL | 17.3974 mL | 34.7947 mL | 86.9868 mL |
| 5 mM | 0.6959 mL | 3.4795 mL | 6.9589 mL | 17.3974 mL | |
| 10 mM | 0.3479 mL | 1.7397 mL | 3.4795 mL | 8.6987 mL | |
| 15 mM | 0.2320 mL | 1.1598 mL | 2.3196 mL | 5.7991 mL | |
| 20 mM | 0.1740 mL | 0.8699 mL | 1.7397 mL | 4.3493 mL | |
| 25 mM | 0.1392 mL | 0.6959 mL | 1.3918 mL | 3.4795 mL | |
| 30 mM | 0.1160 mL | 0.5799 mL | 1.1598 mL | 2.8996 mL | |
| 40 mM | 0.0870 mL | 0.4349 mL | 0.8699 mL | 2.1747 mL | |
| 50 mM | 0.0696 mL | 0.3479 mL | 0.6959 mL | 1.7397 mL | |
| 60 mM | 0.0580 mL | 0.2900 mL | 0.5799 mL | 1.4498 mL | |
| 80 mM | 0.0435 mL | 0.2175 mL | 0.4349 mL | 1.0873 mL | |
| 100 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8699 mL |
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