EZM 2302
Based on 15 publication(s) in Google Scholar
EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression.
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- Pureza: 99.51%
- No. CAS: 1628830-21-6
- Fòrmula: C29H37ClN6O5
- Peso molecular:585.09
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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
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Publications Citing Use of MedChemExpress (MCE) EZM 2302
More- Nat Commun. 2020 Dec 8;11(1):6297. [Abstract]
- Redox Biol. 2024 Sep 6:76:103344. [Abstract]
- Redox Biol. 2024 May 31:73:103212. [Abstract]
- Acta Pharm Sin B. 2026 Jun 18.
- J Clin Invest. 2026 May 15;136(10):e199285. [Abstract]
- Adv Sci (Weinh). 2023 Dec;10(36):e2303484. [Abstract]
- Sci Adv. 2022 Dec 9;8(49):eadd8928. [Abstract]
- Cell Death Dis. 2026 Feb 2;17(1):195. [Abstract]
- Mol Ther Oncol. 2025 Feb 20;33(1):200952. [Abstract]
- Mol Med. 2025 Oct 31;31(1):322. [Abstract]
- Cell Rep. 2025 Jun 25;44(7):115919. [Abstract]
- Br J Pharmacol. 2026 Apr 29. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Exp Cell Res. 2023 Jun 1;427(1):113586. [Abstract]
- Aging (Albany NY). 2020 Jun 2;12(11):10578-10593. [Abstract]
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
IC50: 6 nM (CARM1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2058 | IC50 |
19.47 μM
Compound: 1; EZM2302
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Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 4 days by CCK8 method
Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 4 days by CCK8 method
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[PMID: 38574345] |
| A-375 | IC50 |
12.23 μM
Compound: 1; EZM2302
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Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 4 days by CCK8 method
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 4 days by CCK8 method
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[PMID: 38574345] |
EZM 2302 (0-20 µM; 15 days) shows antiproliferative activity activity with IC50s of >20, >20, 12.2, >20, >20 µM for ZR751, MCF7, LNCAP, PC3, VCAP cells, respectively[1].
EZM 2302 (0-5 µM; 96 h) inhibits PABP1 and SMB methylation in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Parameters of EZM 2302 in CD-1 mouse and Sprague-Dawley rat[1].
| Parameters | IV(CD-1 mouse) | PO(CD-1 mouse) | IV (Sprague-Dawley rat) | PO (Sprague-Dawley rat) |
| Dose (mg/kg) | 2 | 10 | 2 | 10 |
| Blood:plasma ratio | 1.2 | 1.2 | 2.6 | ND |
| Cmax(ng/mL) | 177 | 113 ± 22.4 | ||
| Tmax(h) | 2.00 | 2.00 | ||
| AUC0-last(ng.h/mL) | 767 | 568 | 352 ± 30.6 | 453 ± 89.3 |
| AUC0-inf(ng.h/mL) | 772 | 577 | 372 ± 43.3 | 487 ± 102 |
| t1/2(h) | 4.22 | 4.55 | 6.21 ± 1.65 | 6.64 ± 1.41 |
| Vss(L/kg) | 6.53 | 35.6 ± 1.30 | ||
| CL (mL/min/kg) | 43.2 | 90.5 ± 10.5 | ||
| Fa*Fg (%) | ND | 80.7 | ||
| F (%) | 15.0 | 26.2 ± 5.45 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1628830-21-6
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Appearance Solid
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Peso molecular 585.09
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Fòrmula C29H37ClN6O5
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Color White to off-white
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SMILES
CNC[C@@H](O)COC1=CC=C(Cl)C(C2=NC(N3CC4(CCN(C(OC)=O)CC4)C3)=C(C)C(C5=C(C)ON=C5C)=N2)=C1
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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 1 year -20°C 6 months
Publications (15)
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Journal Impact Factor
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Most Recent
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Nat Commun
2020 Dec 8;11(1):6297. PMID: 33293536 -
Redox Biol
2024 Sep 6:76:103344. PMID: 39265499 -
Redox Biol
ROS-mediated cytoplasmic localization of CARM1 induces mitochondrial fission through DRP1 methylation. [Abstract]2024 May 31:73:103212. PMID: 38838552 -
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J Clin Invest
Targeting RANKL-independent osteoclastogenesis overcomes denosumab resistance in models of ER+ breast cancer bone metastasis. [Abstract]2026 May 15;136(10):e199285. PMID: 42138086 -
Adv Sci (Weinh)
Inhibition of CARM1-Mediated Methylation of ACSL4 Promotes Ferroptosis in Colorectal Cancer. [Abstract]2023 Dec;10(36):e2303484. PMID: 37946697
EZM 2302 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Dec;10(36):e2303484. [Abstract]
MC38 cells were subcutaneously injected into the mice, and tumors were treated with mouse anti‐PD1 antibody and EZM2302 (150 mg/kg, i.p.).
EZM 2302 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Dec;10(36):e2303484. [Abstract]
Malondialdehyde (MDA) levels and relative lipid ROS treated with EZM2302 (150 mg/kg, i.p.).
EZM 2302 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Dec;10(36):e2303484. [Abstract]
HEK293T cells transfected with the indicated plasmids and treated with or without 10 × 10−9 M EZM2302 for 24 h. Immunoprecipitation (IP) with an anti‐Flag antibody and Western blotting with an anti‐Myc antibody were performed to detect the ubiquitination level of ACSL4.
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Sci Adv
2022 Dec 9;8(49):eadd8928. PMID: 36475791 -
Cell Death Dis
Reversible arginine methylation regulates mitochondrial IDH2 activity: coordinated control by CARM1 and KDM3A/4A. [Abstract]2026 Feb 2;17(1):195. PMID: 41629283 -
Mol Ther Oncol
Dual CARM1-and IKZF3-targeting: A novel approach to multiple myeloma therapy synergy between CARM1 inhibition and IMiDs. [Abstract]2025 Feb 20;33(1):200952. PMID: 40123976 -
Mol Med
Context-specific applications of CARM1 inhibitors: functional profiles of EZM2302 and TP-064. [Abstract]2025 Oct 31;31(1):322. PMID: 41174476 -
Cell Rep
Inhibiting UPF1 methylation enhances tumor immunotherapy sensitivity by reducing nonsense-mediated mRNA decay. [Abstract]2025 Jun 25;44(7):115919. PMID: 40570371 -
Br J Pharmacol
Dual pharmacological targeting of coactivator-associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice. [Abstract]2026 Apr 29. PMID: 42055601 -
Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
Exp Cell Res
2023 Jun 1;427(1):113586. PMID: 37030331 -
Aging (Albany NY)
CARM1 promotes non-small cell lung cancer progression through upregulating CCNE2 expression. [Abstract]2020 Jun 2;12(11):10578-10593. PMID: 32487779
EZM 2302 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2020 Jun 2;12(11):10578-10593. [Abstract]
The Western blot results show that EZM2302 (10 nM) inhibits the enzymatic activity of CARM1 and CARM2, leading to significantly reduced H3R17me2a and H3R26me2a levels.
Solvente y solubilidad
DMSO : 100 mg/mL (170.91 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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
Cultured cells in linear/log phase growth are split to a seeding density of 2e5 cells/mL in 2–20mLs of media, depending on the yield required at the end of the growth period. EZM 2302 is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 hours. At the conclusion of each treatment period, cells are harvested by centrifugation (5 minutes, 1200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Male Sprague-Dawley rats (n=3) are treated with a single dose of EZM2302 at 2 mg/kg by intravenous (i.v.) injection and 10 mg/kg by oral gavage administration (p.o.; mouse only), formulated in 5% dextrose in water, pH 3.5. An additional group of rats, cannulated in both the jugular and portal veins are dosed by oral gavage (10 mg/kg, in 0.5% methylcellulose in water). Approximately 110 μL of blood is taken from the animals by retro-orbital bleeding (mouse), tail vein (rat i.v.) or both jugular and portal vein sampling (rat p.o.) at pre-specified time intervals. The 2 h samples are split for parallel determination of blood and plasma concentration[1].
Mice[1]
RPMI-8226 cells are inoculated at 5×106 cells/mouse and treatment began when the mean tumor sizes reach 120 mm3 (28 days post-inoculation). CB-17 SCID Mice are assigned into groups using a randomized block design. EZM2302 or vehicle (0.5% methylcellulose in water) is administered orally BID at a dose volume of 37.5, 75, 150, or 300 mg/kg for 21 days. Body weights are measured twice a week for the duration of the study. Tumor size is measured twice weekly in two dimensions using a caliper, and the volume is expressed in cubic millimeters. Animals are euthanized 3 hours post-final dose, with blood and tissues collected for analysis[1].
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 (279 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
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7091 mL | 8.5457 mL | 17.0914 mL | 42.7285 mL |
| 5 mM | 0.3418 mL | 1.7091 mL | 3.4183 mL | 8.5457 mL | |
| 10 mM | 0.1709 mL | 0.8546 mL | 1.7091 mL | 4.2728 mL | |
| 15 mM | 0.1139 mL | 0.5697 mL | 1.1394 mL | 2.8486 mL | |
| 20 mM | 0.0855 mL | 0.4273 mL | 0.8546 mL | 2.1364 mL | |
| 25 mM | 0.0684 mL | 0.3418 mL | 0.6837 mL | 1.7091 mL | |
| 30 mM | 0.0570 mL | 0.2849 mL | 0.5697 mL | 1.4243 mL | |
| 40 mM | 0.0427 mL | 0.2136 mL | 0.4273 mL | 1.0682 mL | |
| 50 mM | 0.0342 mL | 0.1709 mL | 0.3418 mL | 0.8546 mL | |
| 60 mM | 0.0285 mL | 0.1424 mL | 0.2849 mL | 0.7121 mL | |
| 80 mM | 0.0214 mL | 0.1068 mL | 0.2136 mL | 0.5341 mL | |
| 100 mM | 0.0171 mL | 0.0855 mL | 0.1709 mL | 0.4273 mL |
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