Art. -Nr.: HY-148458

EZH2-IN-14

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EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC₅₀ of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1.

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Reinheit: 98.06%
CAS. Nr.: 1979157-17-9
Formel: C₃₁H₃₉N₇O₂
Molecular Weight:541.69

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

EZH2-IN-14 Chemical Structure

CAS. Nr.: 1979157-17-9

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	16.14 μM Compound: C24; 8	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
A549	IC₅₀	7.48 μM Compound: C24; 8	Synergistic antiproliferative activity against human A549 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay Synergistic antiproliferative activity against human A549 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay	[PMID: 37379621]
BT-549	IC₅₀	15.05 μM Compound: C24; 8	Antiproliferative activity against human BT-549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
BT-549	IC₅₀	4.73 μM Compound: C24; 8	Synergistic antiproliferative activity against human BT-549 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay Synergistic antiproliferative activity against human BT-549 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay	[PMID: 37379621]
HCT-116	IC₅₀	>20 μM Compound: 8; C24	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
HCT-116	IC₅₀	0.92 μM Compound: C24; 8	Synergistic antiproliferative activity against human HCT-116 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay Synergistic antiproliferative activity against human HCT-116 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay	[PMID: 37379621]
HCT-116	IC₅₀	16.95 μM Compound: C24; 8	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
HL-60	IC₅₀	>20 μM Compound: 8; C24	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MDA-MB-231	IC₅₀	>20 μM Compound: 8; C24	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MDA-MB-231	IC₅₀	1.1 μM Compound: C24; 8	Synergistic antiproliferative activity against human MDA-MB-231 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay Synergistic antiproliferative activity against human MDA-MB-231 cells at JQ1 and compound 1:1 ratio incubated for 72 hrs by MTT assay	[PMID: 37379621]
MDA-MB-231	IC₅₀	11.65 μM Compound: C24; 8	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 37379621]
MV4-11	IC₅₀	11.12 μM Compound: 8; C24	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
SU-DHL10	IC₅₀	>20 μM Compound: 8; C24	Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]

In Vitro

EZH2-IN-14 (C24) effectively reduces the H3K27me3 and H3K27me2 marks. EZH2-IN-14 has little effect on the level of EZH2 protein in MDA-MB-468 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

4 μM
Incubation Time:

6 hours, 12 hours, 24 hours, 48 hours
Result:

Reduced the H3K27me3 and H3K27me2 marks.

Chemical Information

CAS. Nr. 1979157-17-9
Appearance Solid
Molecular Weight 541.69
Formel C₃₁H₃₉N₇O₂
Color Off-white to light yellow
SMILES

O=C(C1=CC(C2=CC=C(N3CCN(C(C)C)CC3)N=C2)=CC4=C1C=NN4C(C)C)NCC5=C(C)C=C(C)NC5=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (230.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8461 mL

9.2304 mL

18.4607 mL

5 mM

0.3692 mL

1.8461 mL

3.6921 mL

10 mM

0.1846 mL

0.9230 mL

1.8461 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8461 mL	9.2304 mL	18.4607 mL	46.1519 mL
	5 mM	0.3692 mL	1.8461 mL	3.6921 mL	9.2304 mL
	10 mM	0.1846 mL	0.9230 mL	1.8461 mL	4.6152 mL
	15 mM	0.1231 mL	0.6154 mL	1.2307 mL	3.0768 mL
	20 mM	0.0923 mL	0.4615 mL	0.9230 mL	2.3076 mL
	25 mM	0.0738 mL	0.3692 mL	0.7384 mL	1.8461 mL
	30 mM	0.0615 mL	0.3077 mL	0.6154 mL	1.5384 mL
	40 mM	0.0462 mL	0.2308 mL	0.4615 mL	1.1538 mL
	50 mM	0.0369 mL	0.1846 mL	0.3692 mL	0.9230 mL
	60 mM	0.0308 mL	0.1538 mL	0.3077 mL	0.7692 mL
	80 mM	0.0231 mL	0.1154 mL	0.2308 mL	0.5769 mL
	100 mM	0.0185 mL	0.0923 mL	0.1846 mL	0.4615 mL

Keywords

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EZH2-IN-14

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZH2-IN-14

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EZH2-IN-14 Related Classifications

HY-148458 Related Classifications