Cat. No.: HY-12970B

EPZ020411 dihydrochloride

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

CAS No.: 2095432-47-4
Formula: C₂₅H₄₀Cl₂N₄O₃
Molecular Weight:515.52

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

EPZ020411 dihydrochloride Chemical Structure

CAS No.: 2095432-47-4

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (10)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PRMT6

0.010 μM (IC₅₀)

All Histone Methyltransferase Isoforms :

In Vitro

EPZ020411 dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	AUC_0-inf	T_max	C_max	Bioavailability
Rat^[1]	1 mg/kg	i.v.	19.7 ± 1.0 mL/min/kg	11.1 ± 1.6 L/kg	8.54 ± 1.43 h	846 ± 45 ng·h/mL	/	/	/
Rat^[1]	5 mg/kg	s.c.	/	/	9.19 ± 1.60 h	2775 ± 181 ng·h/mL	0.444 h	844 ± 306 ng/mL	65.6 ± 4.3 %

In Vivo

EPZ020411 (10 mg/kg; intrathecal injection; 1 h before CCI) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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 No. 2095432-47-4
Molecular Weight 515.52
Formula C₂₅H₄₀Cl₂N₄O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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
Cell Death Dis

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

2023 Oct 9;14(10):655. PMID: 37813837
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
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 Jul: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 dihydrochloride 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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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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.

EPZ020411 dihydrochloride

10 Cited Publications

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EPZ020411 dihydrochloride

Publications Citing Use of MedChemExpress (MCE) EPZ020411 dihydrochloride

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (10)

Purity & Documentation

References

Calculators

Help & FAQs

EPZ020411 dihydrochloride Related Classifications

HY-12970B Related Classifications