Art. -Nr.: HY-100757

CPUY074020

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CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC₅₀ of 2.18 μM. CPUY074020 possesses anti-proliferative activity.

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Reinheit: 98.56%
CAS. Nr.: 902279-44-1
Formel: C₂₅H₂₈N₄O₂
Molecular Weight:416.52

Speicherung:

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

CPUY074020 Chemical Structure

CAS. Nr.: 902279-44-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC₅₀ of 2.18 μM. CPUY074020 possesses anti-proliferative activity^[1].

IC₅₀ & Target

EHMT2/G9a/KMT1C

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	3.18 μM Compound: CPUY074020	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
HepG2	IC₅₀	7.93 μM Compound: CPUY074020	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
MCF7	IC₅₀	4.52 μM Compound: CPUY074020	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]

In Vitro

CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis^[1].
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation^[1].

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

Apoptosis Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

2 μM, 4 μM, 8 μM
Incubation Time:

24 hours
Result:

Induced MCF-7 cells apoptosis.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

2.5 μM, 5 μM, 10 μM
Incubation Time:

48 hours
Result:

Dose-dependently de-regulated H3K9 trimethylation.

In Vivo

CPUY074020 exhibits reasonable PK properties, with an oral bioavailability of 55.5% and a T_1/2 value of 4.0 hours at an oral dose of 10 mg/kg^[1].

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

Animal Model:

Mice
Dosage:

10 mg/kg
Administration:

Oral administration
Result:

t_1/2=4.0 hours

Chemical Information

CAS. Nr. 902279-44-1
Appearance Solid
Molecular Weight 416.52
Formel C₂₅H₂₈N₄O₂
Color Brown to dark brown
SMILES

O=C1C2=CC=CC=C2C3=C4C1=C(NCCN5CCCC5)C=C(N6CCCCC6)C4=NO3
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 : 20 mg/mL (48.02 mM; Need ultrasonic; 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

2.4008 mL

12.0042 mL

24.0085 mL

5 mM

0.4802 mL

2.4008 mL

4.8017 mL

10 mM

0.2401 mL

1.2004 mL

2.4008 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 mg/mL (4.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.

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 (278 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]. Chen WL, et al. Discovery, design and synthesis of 6H-anthra[1,9-cd]isoxazol-6-one scaffold as G9a inhibitor through a combination of shape-based virtual screening and structure-based molecular. Bioorg Med Chem. 2016 Nov 15;24(22):6102-6108. [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	2.4008 mL	12.0042 mL	24.0085 mL	60.0211 mL
	5 mM	0.4802 mL	2.4008 mL	4.8017 mL	12.0042 mL
	10 mM	0.2401 mL	1.2004 mL	2.4008 mL	6.0021 mL
	15 mM	0.1601 mL	0.8003 mL	1.6006 mL	4.0014 mL
	20 mM	0.1200 mL	0.6002 mL	1.2004 mL	3.0011 mL
	25 mM	0.0960 mL	0.4802 mL	0.9603 mL	2.4008 mL
	30 mM	0.0800 mL	0.4001 mL	0.8003 mL	2.0007 mL
	40 mM	0.0600 mL	0.3001 mL	0.6002 mL	1.5005 mL

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CPUY074020

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

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

CPUY074020

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

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

CPUY074020 Related Classifications

HY-100757 Related Classifications