TMP269
Based on 22 publication(s) in Google Scholar
TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.16%
- No. CAS: 1314890-29-3
- Fòrmula: C25H21F3N4O3S
- Peso molecular:514.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TMP269
More- Cell Metab. 2021 Dec 7;33(12):2355-2366.e8. [Abstract]
- Cell Host Microbe. 2026 Feb 11;34(2):245-262.e8. [Abstract]
- J Exp Clin Cancer Res. 2025 Feb 24;44(1):67. [Abstract]
- Cell Death Dis. 2023 Jan 18;14(1):38. [Abstract]
- EMBO J. 2024 Nov;43(21):4954-4983. [Abstract]
- EMBO Mol Med. 2026 Jul 21.
- Cell Rep. 2022 Dec 20;41(12):111850. [Abstract]
- Virulence. 2025 Dec;16(1):2495838. [Abstract]
- Eur J Med Chem. 2022 Feb 15:230:114115. [Abstract]
- Commun Biol. 2024 Oct 4;7(1):1257. [Abstract]
- Nutrients. 2023 Jun 15;15(12):2760. [Abstract]
- Int J Mol Sci. 2022 Apr 2;23(7):3980. [Abstract]
- J Enzyme Inhib Med Chem. 2024 Dec;39(1):2406025. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Mar;1870(3):167023. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Biomedicines. 2025 Jan 21;13(2):260. [Abstract]
- Int J Parasitol Drugs Drug Resist. 2026 May 17;31:100649.
- bioRxiv. 2025 Aug 25.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- bioRxiv. 2025 January 31.
- bioRxiv. 2023 Jun 5.
- Patent. US20180263995A1.
Customer Validation & Images
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WB
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IF
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RT-PCR
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ELISA
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Cell Proliferation/Viability Assay
Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC9 23 nM (IC50) |
HDAC7 43 nM (IC50) |
HDAC5 97 nM (IC50) |
HDAC4 157 nM (IC50) |
HDAC8 42000 nM (IC50) |
HDAC6 82000 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
83 μM
Compound: TMP269
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Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
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[PMID: 31201063] |
| LNCaP | GI50 |
21.3 μM
Compound: TMP269
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Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 37633202] |
| RWPE-1 | GI50 |
8 μM
Compound: TMP269
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Antiproliferative activity against human RWPE-1 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human RWPE-1 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 37633202] |
| THP-1 | IC50 |
13 μM
Compound: TMP269
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Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 37979441] |
In Vitro
TMP269 has no impact on the mitochondrial activity and/or the viability of human CD4+ T cells at 10 μM, and may be used as tools to identify the endogenous substrates of the class IIa HDAC enzymes[1]. In IEC-18 intestinal epithelial cells, TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation[2]. As with HDAC4 knockdown, TMP269 significantly enhances cytotoxicity induced by CFZ in MM cell lines, upregulating ATF4 and CHOP and inducing apoptosis. TMP269 does not hyperacetylate histone H3K9 or α-tubulin in MM cell lines, confirming that it has no inhibitory effects on class I or IIb HDACs. In a dosedependent manner, TPM269-induced cytotoxicity is associated with cleavage of caspase-8, -9, -3 and PARP, consistent with apoptosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1314890-29-3
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Appearance Solid
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Peso molecular 514.52
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Fòrmula C25H21F3N4O3S
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Color White to off-white
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SMILES
O=C(NCC1(C2=NC(C3=CC=CC=C3)=CS2)CCOCC1)C4=CC=CC(C5=NOC(C(F)(F)F)=N5)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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Journal Impact Factor
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Most Recent
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Cell Metab
Microbial regulation of hexokinase 2 links mitochondrial metabolism and cell death in colitis. [Abstract]2021 Dec 7;33(12):2355-2366.e8. PMID: 34847376 -
Cell Host Microbe
Enterococcus faecalis-derived lactic acid suppresses macrophage activation to facilitate persistent and polymicrobial wound infections. [Abstract]2026 Feb 11;34(2):245-262.e8. PMID: 41605216 -
J Exp Clin Cancer Res
CD47 blockade reverses resistance to HDAC inhibitor by liberating anti-tumor capacity of macrophages. [Abstract]2025 Feb 24;44(1):67. PMID: 39994810 -
Cell Death Dis
HDAC7/c-Myc signaling pathway promotes the proliferation and metastasis of choroidal melanoma cells. [Abstract]2023 Jan 18;14(1):38. PMID: 36653340
TMP269 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jan 18;14(1):38. [Abstract]
EdU incorporation was analyzed in LV-Control and LV-HDAC7 OCM1/C918 cells treated with TMP269 (20 μM; 48 h). TMP269 partially reversed HDAC7-induced CM cell proliferation.
TMP269 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jan 18;14(1):38. [Abstract]
HDAC7, c-Myc, CDK1, Cyclin B1, CDK2, and Cyclin A2 levels were analyzed by western blotting in LV-Control and LV-HDAC7 OCM1/C918 cells treated with TMP269 (20-60 μM; 48 h). Increasing TMP269 concentrations reduced these protein levels.
TMP269 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jan 18;14(1):38. [Abstract]
LV-Control and LV-HDAC7 OCM1/C918 cells were pretreated with TMP269 (20 μM) for 48 h. Typical pictures (×200) and statistical analysis of the transwell assay. TMP269 partially reversed HDAC7-induced CM cell metastasis.
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EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
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Cell Rep
Lysine crotonylation regulates leucine-deprivation-induced autophagy by a 14-3-3ε-PPM1B axis. [Abstract]2022 Dec 20;41(12):111850. PMID: 36543144
TMP269 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2022 Dec 20;41(12):111850. [Abstract]
14-3-3ε was immunoprecipitated from AML12 cells treated with TMP269 (10 μM; 12 h), and its lysine crotonylation level was assessed. TMP269 increased 14-3-3ε crotonylation.
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Virulence
The inhibitory and anti-inflammatory effects of TMP269 on peste des petits ruminants virus replication. [Abstract]2025 Dec;16(1):2495838. PMID: 40275702
TMP269 purchased from MedChemExpress. Usage Cited in: Virulence. 2025 Dec;16(1):2495838. [Abstract]
PPRV N protein expression was analyzed by western blotting in caprine endometrial epithelial cells treated with TMP269 (1-10 μM; 12 h pretreatment followed by 48 h during PPRV infection). The result demonstrated the potent inhibitory effects of TMP269 on PPRV replication in EECs.
TMP269 purchased from MedChemExpress. Usage Cited in: Virulence. 2025 Dec;16(1):2495838. [Abstract]
Positive infected cells were analyzed in caprine endometrial epithelial cells treated with TMP269 (10 μM; 12 h pretreatment followed by 48 h during PPRV infection), with nuclei stained using DAPI. IF assays in EECs showed a strong inhibitory effect of TMP269 on PPRV replication.
TMP269 purchased from MedChemExpress. Usage Cited in: Virulence. 2025 Dec;16(1):2495838. [Abstract]
PPRV N RNA and the expression of CCL5, CCL7, CXCL8, CCL2, and IL-6 were measured by qRT-PCR in Vero cells treated with TMP269 (10 μM; 12 h pretreatment followed by 48 h during PPRV infection, MOI=0.1). The result demonstrated strong inhibition of PPRV replication by TMP269 and reduced the expression of these pro-inflammatory chemokines and cytokine.
TMP269 purchased from MedChemExpress. Usage Cited in: Virulence. 2025 Dec;16(1):2495838. [Abstract]
CCL5, IL-6, CCL2, and CCL7 concentrations were measured by ELISA in supernatants from Vero cells treated with TMP269 (10 μM; 12 h pretreatment followed by 48 h during PPRV infection, MOI=0.1). TMP269 led to a marked reduction in the expression levels of CCL5 and CCL2, while the expression of CCL7 after TMP269 treatment was even lower than that in uninfected groups (MOCK), suggesting that TMP269 might also reduce some baseline inflammation.
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Eur J Med Chem
Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. [Abstract]2022 Feb 15:230:114115. PMID: 35033824 -
Commun Biol
Selective inhibition of HDAC class IIA as therapeutic intervention for KMT2A-rearranged acute lymphoblastic leukemia. [Abstract]2024 Oct 4;7(1):1257. PMID: 39362994 -
Nutrients
Butyrate Protects Barrier Integrity and Suppresses Immune Activation in a Caco-2/PBMC Co-Culture Model While HDAC Inhibition Mimics Butyrate in Restoring Cytokine-Induced Barrier Disruption. [Abstract]2023 Jun 15;15(12):2760. PMID: 37375664 -
Int J Mol Sci
Butyrate Prevents Induction of CXCL10 and Non-Canonical IRF9 Expression by Activated Human Intestinal Epithelial Cells via HDAC Inhibition. [Abstract]2022 Apr 2;23(7):3980. PMID: 35409339 -
J Enzyme Inhib Med Chem
Synthesis and biological evaluation of ortho-phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases. [Abstract]2024 Dec;39(1):2406025. PMID: 39316378 -
Biochim Biophys Acta Mol Basis Dis
HDAC9 inhibition reduces skeletal muscle atrophy and enhances regeneration in mice with cigarette smoke-induced COPD. [Abstract]2024 Mar;1870(3):167023. PMID: 38218381 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Biomedicines
Butyrate Prevents Obesity Accompanied by HDAC9-Mediated Browning of White Adipose Tissue. [Abstract]2025 Jan 21;13(2):260. PMID: 40002674 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (194.36 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.86 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
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.
Protocolo
Kinase Assay[1]
Dose-response studies are done with ten concentrations in a threefold dilution series from a maximum final compound concentration of 100 μM in the reaction mixture. All assays are based on the same principle as the HDAC9 assay described above: the deacetylation of acetylated or trifluoroacetylated lysine residues on fluorogenic peptide substrates by HDAC. HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 used a substrate based on residues 379-382 of p53 (Arg-His-Lys-Lys(Ac)). For HDAC8, the diacetylated peptide substrate, based on residues 379-382 of p53 (Arg-His-Lys(Ac)-Lys(Ac)), is used. HDAC4, HDAC5, HDAC7 and HDAC9 assays used the class IIa HDAC-specific fluorogenic substrate (Boc-Lys(trifluoroacetyl)-AMC). All reactions are done with 50 μM HDAC substrate in assay buffer (50 mM Tris-HCl, pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA) containing 1% DMSO final concentration; incubated for 2 h at 30°C; and developed with trichostatin A and trypsin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[1]
Human CD4+ T cells are isolated from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plated at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer’s instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25. [Content Brief]
[2]. Sinnett-Smith J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71. [Content Brief]
[3]. Kikuchi S, et al. Class IIa HDAC inhibition enhances ER stress-mediated cell death in multiple myeloma. Leukemia. 2015 Sep;29(9):1918-1927. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9436 mL | 9.7178 mL | 19.4356 mL | 48.5890 mL |
| 5 mM | 0.3887 mL | 1.9436 mL | 3.8871 mL | 9.7178 mL | |
| 10 mM | 0.1944 mL | 0.9718 mL | 1.9436 mL | 4.8589 mL | |
| 15 mM | 0.1296 mL | 0.6479 mL | 1.2957 mL | 3.2393 mL | |
| 20 mM | 0.0972 mL | 0.4859 mL | 0.9718 mL | 2.4294 mL | |
| 25 mM | 0.0777 mL | 0.3887 mL | 0.7774 mL | 1.9436 mL | |
| 30 mM | 0.0648 mL | 0.3239 mL | 0.6479 mL | 1.6196 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4859 mL | 1.2147 mL | |
| 50 mM | 0.0389 mL | 0.1944 mL | 0.3887 mL | 0.9718 mL | |
| 60 mM | 0.0324 mL | 0.1620 mL | 0.3239 mL | 0.8098 mL | |
| 80 mM | 0.0243 mL | 0.1215 mL | 0.2429 mL | 0.6074 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1944 mL | 0.4859 mL |
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