Art. -Nr.: HY-122182

OTS193320

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OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX.

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Reinheit: 99.11%
CAS. Nr.: 2093401-33-1
Formel: C₂₈H₃₀ClN₅O₄
Molecular Weight:536.02

Speicherung:

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

OTS193320 Chemical Structure

CAS. Nr.: 2093401-33-1

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

SUV39H2/KMT1B

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

OTS193320 (0.125-0.5 μM; 24 hours) has growth inhibitory effect on breast cancer cell lines. OTS193320 exhibits a high inhibitory effect against SUV39H2 enzymatic activity (IC₅₀=22.2 nM) and a growth suppressive effect of SUV39H2-positive A549 lung cancer cells (IC₅₀=0.38 μM)^[1].
OTS193320 (0.5 μM; 48 hours) induces apoptosis in breast cancer cells^[1].
OTS193320 (0.125-0.5 μM; 24 hours) causes attenuation of H3K9me3 levels in a dose-dependent manner^[1].
OTS193320 sensitizes breast cancer cells to doxorubicin via attenuation of γ-H2AX. Combination of OTS193320 and doxorubicin (DOX) significantly attenuates cancer cell viability in vitro, compared to single agent treatment of either drug^[1].

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

Cell Viability Assay^[1]

Cell Line:

MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, BT-20 breast cancer cell lines
Concentration:

0-1 μM
Incubation Time:

72 hours
Result:

Had Growth inhibitory effect on MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, and BT-20 breast cancer cell lines with IC₅₀ values from 0.41 to 0.56 μM, respectively.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231 and BT-20 cells
Concentration:

0.5 μM
Incubation Time:

48 hours
Result:

Showed an increase in the number of cells at early- and late-stage apoptosis.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and BT-20 cells
Concentration:

0.125, 0.25, 0.5 μM
Incubation Time:

24 hours
Result:

Caused attenuation of H3K9me3 levels in a dose-dependent manner.

Chemical Information

CAS. Nr. 2093401-33-1
Appearance Solid
Molecular Weight 536.02
Formel C₂₈H₃₀ClN₅O₄
Color Light yellow to yellow
SMILES

O=[N+](C1=CC=C(CN[C@@H]2CC[C@H](NC3=CC4=NC(C5=CC(Cl)=C(OC)C=C5OC)=CN4C=C3)CC2)C=C1)[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 : 62.5 mg/mL (116.60 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

1.8656 mL

9.3280 mL

18.6560 mL

5 mM

0.3731 mL

1.8656 mL

3.7312 mL

10 mM

0.1866 mL

0.9328 mL

1.8656 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: ≥ 6.25 mg/mL (11.66 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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% Corn Oil

Solubility: ≥ 6.25 mg/mL (11.66 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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 (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Theodore Vougiouklakis, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831. [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	1.8656 mL	9.3280 mL	18.6560 mL	46.6400 mL
	5 mM	0.3731 mL	1.8656 mL	3.7312 mL	9.3280 mL
	10 mM	0.1866 mL	0.9328 mL	1.8656 mL	4.6640 mL
	15 mM	0.1244 mL	0.6219 mL	1.2437 mL	3.1093 mL
	20 mM	0.0933 mL	0.4664 mL	0.9328 mL	2.3320 mL
	25 mM	0.0746 mL	0.3731 mL	0.7462 mL	1.8656 mL
	30 mM	0.0622 mL	0.3109 mL	0.6219 mL	1.5547 mL
	40 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1660 mL
	50 mM	0.0373 mL	0.1866 mL	0.3731 mL	0.9328 mL
	60 mM	0.0311 mL	0.1555 mL	0.3109 mL	0.7773 mL
	80 mM	0.0233 mL	0.1166 mL	0.2332 mL	0.5830 mL
	100 mM	0.0187 mL	0.0933 mL	0.1866 mL	0.4664 mL

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OTS193320

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) 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

OTS193320

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) 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

OTS193320 Related Classifications

HY-122182 Related Classifications