1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Epigenetics
  2. Microtubule/Tubulin Apoptosis Histone Demethylase
  3. MY-943

MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research.

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

MY-943 Chemical Structure

MY-943 Chemical Structure

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1 mg USD 190 In-stock
5 mg USD 580 In-stock
10 mg USD 1050 In-stock
25 mg USD 2250 In-stock
50 mg USD 3600 In-stock
100 mg USD 5800 In-stock
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Description

MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research[1].

In Vitro

MY-943 exhibits the anti-proliferative activities against three kinds of cancer cells with IC50 values of 0.019 μM for MGC-803, 0.044 μM for HCT-116 and 0.030 μM for KYSE450[1].
MY-943 (10, 20, 30 nM; 20, 40, 48, 60 h) dose-dependently and time-dependently inhibits the cell viability of MGC-803 and SGC-7901 cells[1].
MY-943 (1, 5, 10 μm; 48 h) dose-dependently weakens the alkylation of β-tubulin in the presence of EBI, and prevents the formation of β-tubulin:EBI adduct band in MGC-803 and SGC-7901 cells[1].
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) concentration-dependently inhibits tubulin polymerization in MGC-803 and SGC-7901 cells[1].
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) dose-dependently induces cell apoptosis[1].
MY-943 dose-dependently down-regulates the expression levels of Bcl-2 and Mcl-1 (anti-apoptotic proteins), and dose-dependently increases the expression levels of cleaved Caspase-3 and Caspase-7[1].
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) dose-dependently down-regulates the expression levels of Weel, CyclinB1 and CDC2, and dose-dependently increases the expression levels of p-Histone H3, H3K4me1 and H3K4me2[1].
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) effectively and dose-dependently induces G2/M phase arrest[1].
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) significantly inhibits the migration ability of gastric cancer cells MGC-803 and SGC-7901[1].

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

Cell Viability Assay[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM
Incubation Time: 20, 40, 48, 60 h
Result: Dose-dependently inhibited the cell viability of MGC-803 and SGC-7901 cells (10, 20, 30 nM; 48 h). Time-dependently inhibited the cell viability of MGC-803 and SGC-7901 cells (10, 20, 30 nM; 20, 40, 60 h).

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 1, 5, 10 μM
Incubation Time: 48 h
Result: Dose-dependently weakened the alkylation of β-tubulin in the presence of EBI, and prevented the formation of β-tubulin:EBI adduct band in MGC-803 and SGC-7901 cells.

Immunofluorescence[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Concentration-dependently inhibited tubulin polymerization in MGC-803 and SGC-7901 cells, thereby destroying the microtubule network.

Immunofluorescence[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: A concentration-dependently made cell nuclei brighten, shrink, and vary in size, and when the concentration was 24 nM for MGC-803 cells or 30 nM for SGC-7901 cells, the nucleus appeared broken, showing the morphological characteristics of apoptotic cells and the proportion of dead cells increased.

Cell Proliferation Assay[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Effectively and dose-dependently induced G2/M phase arrest. After the treatment with 24 nmol/L (MGC-803 cells) or 30 nmol/L (SGC-7901 cells), the percentages of G2/M phase in MGC-803 and SGC-7901 cells were 60% and 74%. While the percentages of G2/M in untreated groups were 33% (MGC-803 cells) and 32% (SGC-7901 cells), respectively.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Down-regulated the expression levels of Bcl-2 and Mcl-1 (anti-apoptotic proteins) in a dose-dependent manner, significantly increased the protein levels of cleaved Caspase-3 and Caspase-7.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Down-regulated the expression levels of the proliferation related proteins Weel and CDC2 in dose-dependent manners, thus leading to the decrease of cdc2 phosphorylation (thr161). While decreased the expression level of CyclinB1 (a G2 phase related protein), and obviously increased the expression level of p-Histone H3 (a M phase marker protein) in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: With the increase of concentrations, increased the expression levels of H3K4me1 and H3K4me2, indicating that inhibited cellular activity of LSD1 in MGC-803 and SGC-7901 cells.

Cell Migration Assay [1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Exhibited significant inhibitory effects on the migratory ability of gastric cancer cells MGC-803 and SGC-7901 cells.
In Vivo

MY-943 (25 mg/kg/day; i.p.; 21 days) significantly inhibits the growth of gastric cancer and greatly reduces the weight and volume of the tumor tissues in mice[1].

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

Animal Model: BALB/c-nu nude mice[1]
Dosage: 25 mg/kg
Administration: 25 mg/kg/day; i.p.; 21 days
Result: Significantly inhibited the growth of gastric cancer and greatly reduced the weight and volume of the tumor tissues.
Molecular Weight

612.76

Formula

C30H36N4O6S2

Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC(N(C(CSC(N2CCN(CC2)C3=CC=C(C=C3)N)=S)=O)CC4=CC(O)=C(C=C4)OC)=CC(OC)=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (163.20 mM; Need ultrasonic; 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 1.6320 mL 8.1598 mL 16.3196 mL
5 mM 0.3264 mL 1.6320 mL 3.2639 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 2.5 mg/mL (4.08 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.08 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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Saline
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 1.6320 mL 8.1598 mL 16.3196 mL 40.7990 mL
5 mM 0.3264 mL 1.6320 mL 3.2639 mL 8.1598 mL
10 mM 0.1632 mL 0.8160 mL 1.6320 mL 4.0799 mL
15 mM 0.1088 mL 0.5440 mL 1.0880 mL 2.7199 mL
20 mM 0.0816 mL 0.4080 mL 0.8160 mL 2.0400 mL
25 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6320 mL
30 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3600 mL
40 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0200 mL
50 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
60 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
80 mM 0.0204 mL 0.1020 mL 0.2040 mL 0.5100 mL
100 mM 0.0163 mL 0.0816 mL 0.1632 mL 0.4080 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.

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MY-943
Cat. No.:
HY-149249
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