Art. -Nr.: HY-A0298

EZH2-IN-2

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EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC₅₀ and a TR-FRET IC₅₀ of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.

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Reinheit: 98.51%
CAS. Nr.: 2238821-31-1
Formel: C₃₆H₄₆N₆O₃
Molecular Weight:610.79

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

EZH2-IN-2 Chemical Structure

CAS. Nr.: 2238821-31-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EZH2

64 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Daudi	GI₅₀	>10 μM Compound: 29	Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
KARPAS-422	GI₅₀	0.05 μM Compound: 29	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Pfeiffer	GI₅₀	0.003 μM Compound: 29	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Raji	GI₅₀	>10 μM Compound: 29	Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SUD4	GI₅₀	3.87 μM Compound: 29	Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SU-DHL-6	GI₅₀	1.1 μM Compound: 29	Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
U2932	GI₅₀	>10 μM Compound: 29	Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]

Chemical Information

CAS. Nr. 2238821-31-1
Appearance Solid
Molecular Weight 610.79
Formel C₃₆H₄₆N₆O₃
Color White to light yellow
SMILES

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(N4CCN(CC5CC5)CC4)N=C3C)=CC(N(C(C6CC6)=O)CC)=C2C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (16.37 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

1.6372 mL

8.1861 mL

16.3722 mL

5 mM

0.3274 mL

1.6372 mL

3.2744 mL

10 mM

0.1637 mL

0.8186 mL

1.6372 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: ≥ 1 mg/mL (1.64 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

Protocol 2

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

Solubility: ≥ 1 mg/mL (1.64 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.64 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 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 (270 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]. LIU, Qing Song, et al. Ezh2 inhibitor and use thereof. WO2018133795A1.

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	1.6372 mL	8.1861 mL	16.3722 mL	40.9306 mL
	5 mM	0.3274 mL	1.6372 mL	3.2744 mL	8.1861 mL
	10 mM	0.1637 mL	0.8186 mL	1.6372 mL	4.0931 mL
	15 mM	0.1091 mL	0.5457 mL	1.0915 mL	2.7287 mL

Keywords

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EZH2-IN-2

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

Heterocyclic Compound 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-2

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

Heterocyclic Compound 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-2 Related Classifications

HY-A0298 Related Classifications