| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C30H36N4O6S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
MY-943 is a potent inhibitor of tubulin polymerization and LSD1 that displays anticancer activity. It induces G2/M phase cell cycle arrest and apoptosis while inhibiting cell migration, and it can be used in gastric cancer research[1]. It is supplied as a light yellow to yellow solid (C30H36N4O6S2, MW 612.76) at 98.01% purity.
Physical & Chemical Properties
| CAS Number | 3043676-46-3 |
|---|---|
| Molecular Formula | C30H36N4O6S2 |
| Molecular Weight | 612.76 g/mol |
| Purity | 98.01% |
| 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 |
| Signaling Pathway | Cell Cycle/DNA Damage; Cytoskeleton; Apoptosis; Epigenetics |
| Solubility | In Vitro: DMSO: 100 mg/mL (163.20 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (163.20 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 2.5 mg/mL (4.08 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (4.08 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | 2.5 mg/mL (4.08 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Against three kinds of cancer cells, MY-943 shows anti-proliferative activity, with IC50 values of 0.019 μM (MGC-803), 0.044 μM (HCT-116), and 0.030 μM (KYSE450)[1]. In MGC-803 and SGC-7901 cells, MY-943 (10, 20, 30 nM; 20, 40, 48, 60 h) inhibits cell viability in a dose- and time-dependent manner[1]. MY-943 (1, 5, 10 μm; 48 h) weakens β-tubulin alkylation in the presence of EBI in a dose-dependent manner, and prevents formation of the β-tubulin:EBI adduct band in MGC-803 and SGC-7901 cells[1]. In MGC-803 and SGC-7901 cells, MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) inhibits tubulin polymerization in a concentration-dependent manner[1]. Cell apoptosis is induced by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) in a dose-dependent manner[1]. Expression levels of Bcl-2 and Mcl-1 (anti-apoptotic proteins) are down-regulated by MY-943 in a dose-dependent manner, while expression levels of cleaved Caspase-3 and Caspase-7 rise dose-dependently[1]. Expression levels of Wee1, CyclinB1 and CDC2 are down-regulated, and those of p-Histone H3, H3K4me1 and H3K4me2 are raised, by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) in a dose-dependent manner[1]. G2/M phase arrest is induced effectively by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) in a dose-dependent manner[1]. Migration of gastric cancer cells MGC-803 and SGC-7901 is significantly inhibited by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h)[1].
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
In mice, MY-943 (25 mg/kg/day; i.p.; 21 days) significantly inhibits gastric cancer growth and greatly reduces the weight and volume of the tumor tissues[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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