1. Epigenetics
    Apoptosis
  2. Histone Methyltransferase
    Apoptosis
  3. EPZ020411 hydrochloride

EPZ020411 hydrochloride 

Cat. No.: HY-12970A Purity: 98.54%
Handling Instructions

EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.

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

EPZ020411 hydrochloride Chemical Structure

EPZ020411 hydrochloride Chemical Structure

CAS No. : 2070015-25-5

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Solution
10 mM * 1 mL in DMSO USD 182 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 275 In-stock
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50 mg USD 715 In-stock
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100 mg USD 1265 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of EPZ020411 hydrochloride:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE EPZ020411 hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer[1][2].

IC50 & Target

PRMT6

0.01 μM (IC50)

PRMT1

0.119 μM (IC50)

PRMT8

0.223 μM (IC50)

In Vitro

EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].

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

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 0-20 μM
Incubation Time: 24 hours
Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM.

Cell Viability Assay[2]

Cell Line: Cultured cochleae cells
Concentration: 20 and 40 μM
Incubation Time: 6 hours
Result: Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Reduced hair cell loss caused by cisplatin treatment.
In Vivo

EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
1.19 Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats[1].

Rats
IV 1 mg/kg
Rats
SC 5 mg/kg
CL (mL/min/kg) 19.7±1.0
Vss (L/kg) 11.1±1.6
t1/2 (h) 8.54±1.43 9.19±1.60
tmax (h) 0.444
Cmax (ng/mL) 844±306
AUC0-τ (h·ng/mL) 745±34 2456±135
AUC0-inf (h·ng/mL) 846±45 2775±181
F (%) 65.6±4.3

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

Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity model[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg once
Result: Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
Molecular Weight

479.06

Formula

C25H39ClN4O3

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.37 mM; Need ultrasonic)

H2O : 20 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0874 mL 10.4371 mL 20.8742 mL
5 mM 0.4175 mL 2.0874 mL 4.1748 mL
10 mM 0.2087 mL 1.0437 mL 2.0874 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 65 mg/mL (135.68 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.54%

References
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Product Name:
EPZ020411 hydrochloride
Cat. No.:
HY-12970A
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