EPZ020411 hydrochloride |
Catalog No.GC36000
One-Click Copy Product Info
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EPZ020411 hydrochloride is a highly selective, orally bioavailable inhibitor of protein arginine methyltransferase 6 (PRMT6), with an IC50 value of 10nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070015-25-5
Sample solution is provided at 25 µL, 10mM.
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EPZ020411 hydrochloride is a highly selective, orally bioavailable inhibitor of protein arginine methyltransferase 6 (PRMT6), with an IC50 value of 10nM[1]. PRMT6 regulates gene expression by catalyzing asymmetric dimethylation of histone H3 at arginine 2 (H3R2) and plays critical roles in stem cell function regulation, proliferation control, and differentiation[2]. EPZ020411 hydrochloride exhibits selectivity for PRMT6 over PRMT1 and PRMT8 and is commonly used in studies of epigenetic regulation, cancer, and hearing loss protection[3,4].
In vitro, treatment of mouse microglial BV2 cells with EPZ020411 hydrochloride (1, 10, 20, 50, 100, 1000μM) for 24h showed that concentrations of 50μM and above significantly inhibited BV2 cell viability[5]. EPZ020411 (10μM) treatment of primary mouse cortical neurons co-overexpressing HTT 548-17Q and EGFP-PRMT6 for 24h reversed the PRMT6 overexpression-induced increase in huntingtin (HTT) arginine methylation levels[6]. EPZ020411 hydrochloride (4μM) treatment of mismatch repair (MMR)-proficient colorectal cancer SW480 cells for 24h significantly attenuated the assembly of MutSα and MutSβ complexes[7].
In vivo, EPZ020411 hydrochloride (10mg/kg; once daily) administered via intraperitoneal injection to BALB/c mice bearing subcutaneous xenografts of microsatellite stable (MSS) murine colorectal cancer CT26 cells for 3 weeks significantly inhibited tumor growth[7].
References:
[1] MITCHELL L H, DREW A E, RIBICH S A, et al. Aryl pyrazoles as potent inhibitors of arginine methyltransferases: identification of the first PRMT6 tool compound[J]. ACS Medicinal Chemistry Letters, 2015, 6(6): 655-659.
[2] OKUNO K, AKIYAMA Y, SHIMADA S, et al. Asymmetric dimethylation at histone H3 arginine 2 by PRMT6 in gastric cancer progression[J]. Carcinogenesis, 2019, 40(1): 15-26.
[3] WANG J, XIAO Z, LI P, et al. PRMT6-CDC20 facilitates glioblastoma progression via the degradation of CDKN1B[J]. Oncogene, 2023, 42(14): 1088-1100.
[4] LI J, LIU C, QIU S, et al. Epigenetic modifications in sensorineural hearing loss: protective mechanisms and therapeutic potential[J]. Current Medical Science, 2025, 45(3): 415-429.
[5] HUA T, KONG E, ZHANG H, et al. PRMT6 deficiency or inhibition alleviates neuropathic pain by decreasing glycolysis and inflammation in microglia[J]. Brain, Behavior, and Immunity, 2024, 118: 101-114.
[6] MIGAZZI A, SCARAMUZZINO C, ANDERSON E N, et al. Huntingtin-mediated axonal transport requires arginine methylation by PRMT6[J]. Cell Reports, 2021, 35(2).
[7] DUAN J, CHEN T, LI Q, et al. Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer[J]. Journal for ImmunoTherapy of Cancer, 2025, 13(3): e010639.
| Cell experiment [1]: | |
Cell lines | MMR-proficient cell line SW480 |
Preparation Method | SW480 cells were treated with 4μM EPZ020411 hydrochloride for 24h, then cells were lysed and immunoprecipitated with an anti-MSH2 antibody, followed by immunoblotting with anti-MSH3 and anti-MSH6 antibodies to assess the assembly of MutSα and MutSβ complexes. |
Reaction Conditions | 4µM; 24h |
Applications | Treatment with EPZ020411 hydrochloride significantly reduced the assembly of the MutSα and MutSβ complexes. |
| Animal experiment [1]: | |
Animal models | BALB/c mice bearing subcutaneous CT26 tumors |
Preparation Method | BALB/c mice bearing subcutaneous CT26 tumors were administered with EPZ020411 hydrochloride (10mg/kg) via intraperitoneal injection once daily for 3 weeks, then tumor weight was examined and calculated. |
Dosage form | 10mg/kg; once daily; 3 weeks; i.p. |
Applications | Treatment with EPZ020411 hydrochloride significantly inhibited tumor growth. |
References: | |
| Cas No. | 2070015-25-5 | SDF | |
| Canonical SMILES | CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2.Cl[H] | ||
| Formula | C25H39ClN4O3 | M.Wt | 479.06 |
| Solubility | DMSO: 50 mg/mL (104.37 mM); Water: ≥ 41 mg/mL (85.58 mM) | Storage | Store at 4°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0874 mL | 10.4371 mL | 20.8742 mL |
| 5 mM | 417.5 μL | 2.0874 mL | 4.1748 mL |
| 10 mM | 208.7 μL | 1.0437 mL | 2.0874 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)