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

OTS193320 

Cat. No.: HY-122182 Purity: 98.12%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

OTS193320 Chemical Structure

OTS193320 Chemical Structure

CAS No. : 2093401-33-1

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Solution
10 mM * 1 mL in DMSO USD 448 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 448 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 620 In-stock
25 mg USD 1250 In-stock
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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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].

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.
Molecular Weight

536.02

Appearance

Solid

Formula

C28H30ClN5O4
CAS No.
SMILES

O=[N+](C1=CC=C(CN[[email protected]@H]2CC[[email protected]](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)

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
10 mM 0.1866 mL 0.9328 mL 1.8656 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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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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