2. Epigenetics NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Histone Methyltransferase Reactive Oxygen Species (ROS) Apoptosis
  4. EPZ020411 dihydrochloride

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

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of EPZ020411 dihydrochloride:

Other Forms of EPZ020411 dihydrochloride:

EPZ020411 dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3][4][5].

    IC50 & Target[1]

    PRMT6

    0.010 μM (IC50)

    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.

    EPZ020411 dihydrochloride Related Antibodies

    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 Vss T1/2 AUC0-inf Tmax Cmax 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.
    Molecular Weight

    515.52

    Formula

    C25H40Cl2N4O3
    CAS No.
    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.
    Purity & Documentation
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    EPZ020411 dihydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    EPZ0204112095432-47-4EPZ 020411EPZ-020411Histone MethyltransferaseReactive Oxygen Species (ROS)ApoptosisBV2 microglial cellsU87 cellscGAS-STING signalingPRMT6HIF-1αA375 cellsHCT116 cellshistone H3R2glioblastomaLN229 cellsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    EPZ020411 dihydrochloride
    Cat. No.:
    HY-12970B
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.