2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. OTS193320

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 (DOX; 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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OTS193320 Chemical Structure

OTS193320 Chemical Structure

CAS No. : 2093401-33-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

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 (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX[1].

IC50 & Target[1]

SUV39H2/KMT1B

 

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.

OTS193320 Related Antibodies

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.
Molecular Weight

536.02

Formula

C28H30ClN5O4
CAS No.
Appearance

Solid

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8656 mL 9.3280 mL 18.6560 mL
5 mM 0.3731 mL 1.8656 mL 3.7312 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, 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.

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  • Dilution Calculator

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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: ≥ 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.

    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% 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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, 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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OTS1933202093401-33-1OTS 193320OTS-193320Histone MethyltransferaseApoptosisSUV39H2methyltransferasehistone H3 lysine 9 tri-methylationbreast cancerDoxorubicinDOXγ-H2AXMCF-7SK-BR-3ZR-75-1T-47DMDA-MB-231BT-20Inhibitorinhibitorinhibit

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