Art. -Nr.: HY-12970

EPZ020411

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

EPZ020411 is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC₅₀ of 0.010 μM. EPZ020411 blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma.

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Reinheit: 98.07%
CAS. Nr.: 1700663-41-7
Formel: C₂₅H₃₈N₄O₃
Molecular Weight:442.59

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

EPZ020411 Chemical Structure

CAS. Nr.: 1700663-41-7

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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 (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PRMT6

0.010 μM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.637 μM Compound: EPZ020411	Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method	[PMID: 26101569]
A-375	IC₅₀	7.1 μM Compound: EPZ020411	Inhibition of PRMT1 in human A375 cells assessed as effect on monomethyl RGG motif methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method Inhibition of PRMT1 in human A375 cells assessed as effect on monomethyl RGG motif methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method	[PMID: 26101569]
HCC827	IC₅₀	>100 μM Compound: EPZ020411	Antiproliferative activity against human HCC827 cells for 3 days by MTT assay Antiproliferative activity against human HCC827 cells for 3 days by MTT assay	[PMID: 36566712]
HCC827	IC₅₀	4.15 μM Compound: EPZ020411	Antiproliferative activity against human HCC827 cells for 7 days by MTT assay Antiproliferative activity against human HCC827 cells for 7 days by MTT assay	[PMID: 36566712]
HCC827	IC₅₀	8.57 μM Compound: EPZ020411	Antiproliferative activity against human HCC827 cells for 5 days by MTT assay Antiproliferative activity against human HCC827 cells for 5 days by MTT assay	[PMID: 36566712]
MDA-MB-435	IC₅₀	1.1 μM Compound: EPZ020411	Antiproliferative activity against human MDA-MB-435 cells for 7 days by MTT assay Antiproliferative activity against human MDA-MB-435 cells for 7 days by MTT assay	[PMID: 36566712]
MDA-MB-435	IC₅₀	90.43 μM Compound: EPZ020411	Antiproliferative activity against human MDA-MB-435 cells for 5 days by MTT assay Antiproliferative activity against human MDA-MB-435 cells for 5 days by MTT assay	[PMID: 36566712]
MDA-MB-435	IC₅₀	94.65 μM Compound: EPZ020411	Antiproliferative activity against human MDA-MB-435 cells for 3 days by MTT assay Antiproliferative activity against human MDA-MB-435 cells for 3 days by MTT assay	[PMID: 36566712]

In Vitro

EPZ020411 potently inhibits purified PRMT6 enzyme with an IC₅₀ of 0.010 μM, and exhibits over 100-fold selectivity against a variety of other arginine methyltransferases^[1].
EPZ020411(at concentrations greater than 0.01 μM for 48 h) inhibits PRMT6-mediated H3R2me2a modification in PRMT6-overexpressing A375 cells, with an IC₅₀ of 0.637 ± 0.241 μM^[1].
EPZ020411 (1-1000 μM; 24 h) reduces the viability of BV2 microglial cells at concentrations of 50, 100 and 1000 μM, while concentrations of 1, 10 and 20 μM do not alter cell viability^[2].
EPZ020411 (2-4 μM; 14 days) reduces the cell viability of HCT116, HT29, SW480, MC38 and CT26 colorectal cancer (CRC) cell lines, with the maximal effect observed at 4 μM^[3].
EPZ020411 (40 μM) protects hair cells in postnatal day 2 mouse cochlear explants from cisplatin-induced death and significantly increases hair cell survival rates across all cochlear turns^[4].
EPZ020411 (20-40 μM; 48 h) potently inhibits the invasive ability of human glioblastoma U87 and LN229 cells in a concentration-dependent manner^[5].

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

Western Blot Analysis^[3]

Cell Line:

SW480 human CRC cells
Concentration:

2, 4 μM (48 h incubation)
Incubation Time:

48 h
Result:

Stimulated phosphorylation of STAT1 and IRF3 in SW480 cells.

Cell Invasion Assay^[5]

Cell Line:

human glioblastoma U87, human glioblastoma LN229
Concentration:

20 μM, 40 μM
Incubation Time:

48 h (pretreatment prior to assay)
Result:

Reduced invasive cell numbers in U87 and LN229 cells at 20 μM.
Further reduced invasive cell numbers in both cell lines at 40 μM, with statistical significance relative to untreated cells (****p < 0.0001 for U87; ***p < 0.001 for LN229).

Western Blot Analysis^[5]

Cell Line:

human glioblastoma U87, human glioblastoma LN229
Concentration:

20 μM, 40 μM
Incubation Time:

48 h
Result:

Reduced global H3R2me2a levels in both U87 and LN229 cells relative to untreated cells.
Increased TRAF6 protein expression in both U87 and LN229 cells relative to untreated cells.

In Vivo

EPZ020411 (10 mg/kg; intrathecal injection; 1 h before CCI) attenuates CCI-induced neuropathic pain, microglial activation, neuroinflammation and glycolysis in the spinal dorsal horn of mice^[2].
EPZ020411 (10 mg/kg; i.p.; once daily; for 3 consecutive weeks) significantly inhibits the growth of subcutaneous CT26 MSS colorectal cancer xenografts in BALB/c mice^[3].
EPZ020411 (10 mg/kg; i.p.; daily; for 5 consecutive weeks) slightly reduces the tumor burden of microsatellite-stable colorectal cancer induced by AOM/DSS in C57BL/6 mice^[3].
EPZ020411 (administered via transtympanic route; single dose) significantly attenuates neomycin-induced chronic hearing loss in 5-day-old C57BL/6 mice and protects the survival of hair cells in the middle and basal turns of the cochlea^[4]
EPZ020411 (10 mg/kg; i.p.; single administration) significantly attenuates acute hearing loss induced by neomycin combined with furosemide in 28-day-old C57BL/6 mice, maintains hair cell survival, and inhibits cochlear cell apoptosis and reactive oxygen species production^[4].

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

Animal Model:

C57BL/6 (5 days old, neomycin-induced chronic ototoxicity model)^[4]
Dosage:

10 mM (1 μl)
Administration:

trans-tympanic; single dose
Result:

Showed significantly reduced ABR and DPOAE threshold elevation at all tested frequencies (4, 8, 16, 24, 32 kHz) compared to saline-pretreated ears.
Increased myosin 7a-positive hair cell survival significantly in the middle and basal cochlear turns relative to neomycin-only controls.

Animal Model:

C57BL/6 (postnatal day 28, cisplatin-induced ototoxicity model)^[4]
Dosage:

10 mM (5 μl)
Administration:

trans-tympanic; single dose
Result:

Showed significantly reduced ABR and DPOAE threshold elevation at all tested frequencies (4, 8, 16, 24, 32 kHz) at days 4, 7, and 14 post-cisplatin compared to saline-pretreated ears.
Increased myosin 7a-positive hair cell survival significantly in the middle and basal cochlear turns relative to cisplatin-only controls.
Reduced caspase 3/7-positive cells in the middle turn from 22.01 ± 4.435 to 4.018 ± 3.684 per 200 μm.
Reduced MitoSox-Red-positive cells in the middle turn from 43.62 ± 6.740 to 0.9616 ± 0.9760 per 200 μm.

Chemical Information

CAS. Nr. 1700663-41-7
Appearance Solid
Molecular Weight 442.59
Formel C₂₅H₃₈N₄O₃
Color Off-white to light yellow
SMILES

CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (10)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

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
Brain

HSV-1 reactivation results in post-herpetic neuralgia by upregulating Prmt6 and inhibiting cGAS-STING. [Abstract]

2024 Jul 5;147(7):2552-2565. PMID: 38366606
J Immunother Cancer

Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. [Abstract]

2025 Mar 13;13(3):e010639. PMID: 40086819
Cell Death Dis

PRMT6 methylation of STAT3 regulates tumor metastasis in breast cancer. [Abstract]

2023 Oct 9;14(10):655. PMID: 37813837
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
J Transl Med

PRMT6 promotes colorectal cancer progress via activating MYC signaling. [Abstract]

2025 Jan 16;23(1):74. PMID: 39819457
J Transl Med

KLF4 regulates trophoblast function and associates with unexplained recurrent spontaneous abortion. [Abstract]

2024 Oct 10;22(1):922. PMID: 39390495
EMBO Rep

Arginine methylation of SIRT7 couples glucose sensing with mitochondria biogenesis. [Abstract]

2018 Dec;19(12):e46377. PMID: 30420520
Bioorg Chem

Discovery of a first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6). [Abstract]

2024 May 10:148:107439. PMID: 38754310
Exp Cell Res

PRMT6 functionally associates with PRMT5 to promote colorectal cancer progression through epigenetically repressing the expression of CDKN2B and CCNG1. [Abstract]

2022 Nov 16;422(1):113413. PMID: 36400182

EPZ020411 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]

EPZ020411(PRMT6i; 200-1000 nM) in combination with GSK591(PRMT5i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 4.76 mg/mL (10.75 mM; ultrasonic and adjust pH to 7 with 1 M HCl; 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

2.2594 mL

11.2971 mL

22.5943 mL

5 mM

0.4519 mL

2.2594 mL

4.5189 mL

10 mM

0.2259 mL

1.1297 mL

2.2594 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.65 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.65 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.65 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.

Working Solution

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.

Protocol 1

Add each solvent one by one: Saline

Solubility: 4.5 mg/mL (10.17 mM); Clear solution; Need ultrasonic

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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]. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound. ACS Med Chem Lett. 2015;6(6):655-659. Published 2015 Apr 6. [Content Brief]

[2]. Hua T, et al. PRMT6 deficiency or inhibition alleviates neuropathic pain by decreasing glycolysis and inflammation in microglia. Brain Behav Immun. 2024;118:101-114. [Content Brief]

[3]. Duan J, et al. Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. J Immunother Cancer. 2025;13(3):e010639. Published 2025 Mar 13. [Content Brief]

[4]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020;10(1):133-150. Published 2020 Jan 1. [Content Brief]

[5]. Wang J, et al. PRMT6 facilitates EZH2 protein stability by inhibiting TRAF6-mediated ubiquitination degradation to promote glioblastoma cell invasion and migration. Cell Death Dis. 2024;15(7):524. Published 2024 Jul 23. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2594 mL	11.2971 mL	22.5943 mL	56.4857 mL
	5 mM	0.4519 mL	2.2594 mL	4.5189 mL	11.2971 mL
	10 mM	0.2259 mL	1.1297 mL	2.2594 mL	5.6486 mL

EPZ020411

10 Cited Publications

100 mg Angebot einholen

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EPZ020411

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EPZ020411

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EPZ020411

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EPZ020411

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EPZ020411 Related Classifications

Art. -Nr.: HY-12970