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OTS193320

Cat No.:V41059 Purity: ≥98%
OTS193320 is an imidazo[1,2-a]pyridine compound and an inhibitor (blocker/antagonist) of SUV39H2 methyltransferase activity.
OTS193320
OTS193320 Chemical Structure CAS No.: 2093401-33-1
Product category: Apoptosis
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
OTS193320 is an imidazo[1,2-a]pyridine compound and an inhibitor (blocker/antagonist) of SUV39H2 methyltransferase activity. OTS193320 reduces global histone H3 lysine 9 trimethylation levels and triggers apoptotic cell death in breast cancer cells. The combination of OTS193320 and Doxorubicin resulted in a reduction in γ-H2AX levels and cancer cell viability compared to single agents OTS193320 or DOX.
Biological Activity I Assay Protocols (From Reference)
Targets
SUV39H2/KMT1B
ln Vitro
OTS193320 (0.125-0.5 μM; 24 hours) prevents breast cancer cell lines from proliferating. SUV39H2-positive A549 lung cancer cells have growth inhibited by OTS193320 (IC50=0.38 μM)[1]. OTS193320 (0.5 μM; 48 hours) causes breast cancer cells to undergo apoptosis [1]. In a dose-dependent manner, OTS193320 (0.125-0.5 μM; 24 hours) lowers H3K9me3 levels [1]. OTS193320 attenuates γ-H2AX, which makes breast cancer cells more susceptible to doxorubicin. When compared to single agent therapy with either agent, the combination of OTS193320 and doxorubicin dramatically decreased cancer cell viability in vitro [1].
Cell Assay
Cell Viability Assay[1]
Cell Types: MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, BT-20 breast cancer cell lines
Tested Concentrations: 0-1 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: 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 Types: MDA-MB-231 and BT-20 cells
Tested Concentrations: 0.5 μM
Incubation Duration: 48 hrs (hours)
Experimental Results: demonstrated an increase in the number of cells at early- and late-stage apoptosis.

Western Blot Analysis[1]
Cell Types: MDA-MB-231 and BT-20 cells
Tested Concentrations: 0.125, 0.25, 0.5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Caused attenuation of H3K9me3 levels in a dose-dependent manner.
References
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H30CLN5O4
Molecular Weight
536.02
CAS #
2093401-33-1
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
ClC1C(=CC(=C(C=1)C1=CN2C=CC(=CC2=N1)NC1CCC(CC1)NCC1C=CC(=CC=1)[N+](=O)[O-])OC)OC
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 62.5 mg/mL (116.60 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 6.25 mg/mL (11.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 6.25 mg/mL (11.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.1866 mL 0.9328 mL 1.8656 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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