EPZ020411 hydrochloride

Name: EPZ020411 hydrochloride
Brand: MedChemExpress
SKU: HY-12970A
Rating: 5.0 (8 reviews)

Cat. No.: HY-12970A Purity: 98.15%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2070015-25-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 182	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 182	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 715	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1265	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of EPZ020411 hydrochloride:

EPZ020411 Get quote

7 Publications Citing Use of MCE EPZ020411 hydrochloride

•Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]

Proliferation Assay

: EPZ020411 hydrochloride 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.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (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
V_ss (L/kg)	11.1±1.6
t_1/2 (h)	8.54±1.43	9.19±1.60
t_max (h)		0.444
C_max (ng/mL)		844±306
AUC_0-τ (h·ng/mL)	745±34	2456±135
AUC_0-inf (h·ng/mL)	846±45	2775±181
F (%)		65.6±4.3

MedChemExpress (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.

2070015-25-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](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, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (104.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

0.1 M HCL : 50 mg/mL (104.37 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

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

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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 (5.22 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.22 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.

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: PBS
Solubility: 25 mg/mL (52.19 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.15%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (252 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

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

[2]. 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 Jan 1;10(1):133-150. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO / 0.1 M HCL	1 mM	2.0874 mL	10.4371 mL	20.8742 mL	52.1855 mL
	5 mM	0.4175 mL	2.0874 mL	4.1748 mL	10.4371 mL
	10 mM	0.2087 mL	1.0437 mL	2.0874 mL	5.2186 mL
	15 mM	0.1392 mL	0.6958 mL	1.3916 mL	3.4790 mL
	20 mM	0.1044 mL	0.5219 mL	1.0437 mL	2.6093 mL
	25 mM	0.0835 mL	0.4175 mL	0.8350 mL	2.0874 mL
	30 mM	0.0696 mL	0.3479 mL	0.6958 mL	1.7395 mL
	40 mM	0.0522 mL	0.2609 mL	0.5219 mL	1.3046 mL
DMSO / 0.1 M HCL	50 mM	0.0417 mL	0.2087 mL	0.4175 mL	1.0437 mL
	60 mM	0.0348 mL	0.1740 mL	0.3479 mL	0.8698 mL
	80 mM	0.0261 mL	0.1305 mL	0.2609 mL	0.6523 mL
	100 mM	0.0209 mL	0.1044 mL	0.2087 mL	0.5219 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.