Art. -Nr.: HY-111109

EZM 2302

14 Cited Publications

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Based on 14 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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Reinheit: 99.51%
CAS. Nr.: 1628830-21-6
Formel: C₂₉H₃₇ClN₆O₅
Molecular Weight:585.09

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

EZM 2302 Chemical Structure

CAS. Nr.: 1628830-21-6

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 6 nM (CARM1)^[1]

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2058	IC₅₀	19.47 μM Compound: 1; EZM2302	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	[PMID: 38574345]
A-375	IC₅₀	12.23 μM Compound: 1; EZM2302	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	[PMID: 38574345]

In Vitro

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.

In Vivo

EZM 2302 (37.5, 75, 150, 300 mg/kg; p.o.; twice daily for 21 days) shows anti-tumor activity in mouse^[1].
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
C_max(ng/mL)		177		113 ± 22.4
T_max(h)		2.00		2.00
AUC_0-last(ng.h/mL)	767	568	352 ± 30.6	453 ± 89.3
AUC_0-inf(ng.h/mL)	772	577	372 ± 43.3	487 ± 102
t_1/2(h)	4.22	4.55	6.21 ± 1.65	6.64 ± 1.41
V_ss(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

CD-1 mouse and Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1628830-21-6
Appearance Solid
Molecular Weight 585.09
Formel C₂₉H₃₇ClN₆O₅
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

All In Vivo Efficacy StudyFlow CytometryIPWB

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Journal Impact Factor

Nat Commun

Pontin arginine methylation by CARM1 is crucial for epigenetic regulation of autophagy. [Abstract]

2020 Dec 8;11(1):6297. PMID: 33293536
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.
J Clin Invest

2026 May 15;136(10):e199285. PMID: 42138086
Sci Adv

Arginine methylation of BRD4 by PRMT2/4 governs transcription and DNA repair. [Abstract]

2022 Dec 9;8(49):eadd8928. PMID: 36475791
Redox Biol

CARM1 phosphorylation at S595 by p38γ MAPK drives ROS-mediated cellular senescence. [Abstract]

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
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
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
Cell Rep

Inhibiting UPF1 methylation enhances tumor immunotherapy sensitivity by reducing nonsense-mediated mRNA decay. [Abstract]

2025 Jun 25;44(7):115919. PMID: 40570371
Mol Med

Context-specific applications of CARM1 inhibitors: functional profiles of EZM2302 and TP-064. [Abstract]

2025 Oct 31;31(1):322. PMID: 41174476
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
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.
Exp Cell Res

YBX2 modulates mRNA stability via interaction with YTHDF2 in endometrial cancer cells. [Abstract]

2023 Jun 1;427(1):113586. PMID: 37030331
Mol Carcinog

PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]

2023 Aug;62(8):1119-1135. PMID: 37144835

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7091 mL

8.5457 mL

17.0914 mL

5 mM

0.3418 mL

1.7091 mL

3.4183 mL

10 mM

0.1709 mL

0.8546 mL

1.7091 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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.

Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

EZM 2302

14 Cited Publications

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EZM 2302

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) EZM 2302

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZM 2302

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) EZM 2302

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZM 2302 Related Classifications

HY-111109 Related Classifications