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| Targets |
MY-943 targets two distinct molecular entities: (1) beta-tubulin at the colchicine binding site, thereby inhibiting tubulin polymerization and disrupting microtubule network formation; and (2) LSD1, a histone demethylase that regulates epigenetic gene expression. This dual targeting disrupts both mitotic spindle formation and epigenetic regulation.
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| ln Vitro |
MY-943 exhibits anti-proliferative action against MGC-803 cells, HCT-116 cells, and KYSE450 cells, with IC50 values of 0.019 μM, 0.044 μM, and 0.030 μM, respectively [1]. MY-943 (10, 20, 30 nM; 20, 40, 48, and 60 h) suppresses MGC-803 and SGC-7901 cells' ability to proliferate in a dose- and time-dependent manner [1]. MY-943 (1, 5, 10 μM; 48 h) inhibits the formation of EBI adduct bands in MGC-803 and SGC-7901 cells and dose-dependently attenuates β-tubulin alkylation in the presence of EBI [1]. In MGC-803 and SGC-7901 cells, MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) concentration-dependently suppresses tubulin polymerization [1]. In a dose-dependent manner, MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) promotes apoptosis [1]. MY-943 elevates the expression levels of cleaved caspase-3 and caspase-7 in a dose-dependent manner while dose-dependently downregulating the expression levels of anti-apoptotic proteins Bcl-2 and Mcl-1 [1]. Weel, Cyclin B1, and CDC2 expression levels are dose-dependently down-regulated by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h), while the expression levels of p-histone H3, H3K4me1, and H3K4me2 are dose-dependently increased[1]. G2/M phase arrest is potently and dose-dependently induced by MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) [1]. The capacity of MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) to strongly inhibit the migration of MGC-803 and SGC-7901 gastric cancer cells has been shown [1].
MY-943 exhibits low nanomolar antiproliferative activity against 14 cancer cell lines, with IC50 values of 0.019 microM (MGC-803), 0.044 microM (HCT-116), and 0.030 microM (KYSE450), and ranging from 0.019 to 0.253 microM across other lines. It dose-dependently induces accumulation of H3K4me1/2 and H3K9me2 (LSD1 inhibition markers), induces G2/M phase arrest, promotes apoptosis, and suppresses cell migration. |
| ln Vivo |
MY-943 (25 mg/kg/day; i.p.; 21 days) dramatically decreased the weight and volume of tumor tissue in mice and significantly slowed the growth of gastric cancer in mice [1].
In an in situ gastric cancer mouse model, MY-943 effectively reduced both the weight and volume of gastric tumors without obvious toxicity. The in vivo anti-gastric cancer efficacy was demonstrated with no significant adverse effects reported, indicating a favorable therapeutic window for this dual inhibitor. |
| Enzyme Assay |
A standard tubulin polymerization inhibition assay involves incubating purified tubulin (1-2 mg/mL) in GTP-containing buffer (80 mM PIPES, pH 6.9, 2 mM MgCl2, 0.5 mM EGTA) with MY-943 at varying concentrations (0.1-10 microM). The reaction is initiated by warming to 37degC, and tubulin polymerization is monitored spectrophotometrically at 340 nm for 30-60 minutes. A decrease in absorbance indicates inhibition of microtubule formation.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MGC-803 and SGC-7901 cells Tested Concentrations: 10, 20, 30 nM Incubation Duration: 20, 40, 48, 60 h Experimental Results: Dose-dependently inhibited the cell viability of MGC-803 and Time-dependently inhibited the cell viability of MGC-803 and SGC-7901 cells(10, 20, 30 nM; 48 h). Western Blot Analysis[1] Cell Types: MGC-803 and SGC-7901 cells Tested Concentrations: 1, 5, 10 μM Incubation Duration: 48 h Experimental Results: 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 Types: MGC-803 and SGC-7901 cells Tested Concentrations: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells Incubation Duration: 48 h Experimental Results: Concentration-dependently inhibited tubulin polymerization in MGC-803 and SGC-7901 cells, thereby destroying the microtubule network. Immunofluorescence[1] Cell Types: MGC-803 and SGC- 7901 cells Tested Concentrations: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 2 For LSD1 activity assays, standard protocols involve incubating recombinant LSD1 enzyme (10-50 nM) with a biotinylated histone H3 peptide substrate (1-10 microM) and varying concentrations of MY-943 (0.1-10 microM) in assay buffer (50 mM Tris-HCl, pH 8.0, 50 mM NaCl, 1 mM DTT). After 30-60 minutes at 37degC, demethylation is detected using a specific antibody against unmethylated H3K4 or by mass spectrometry. |
| Animal Protocol |
Animal/Disease Models: BALB/c-nu nude mice[1]
Doses: 25 mg/kg Route of Administration: 25 mg/kg/day; ip; 21 days Experimental Results: Dramatically inhibited the growth of gastric cancer and greatly decreased the weight and volume of the tumor tissues. For in vivo efficacy studies, standard protocols involve establishing an in situ gastric cancer model in nude mice via orthotopic implantation of MGC-803 cells. Mice are treated with MY-943 (e.g., 5-20 mg/kg) by oral gavage or intraperitoneal injection daily for 2-4 weeks. Tumor weight and volume are measured at endpoint, and tumor tissues are analyzed for proliferation markers (Ki-67), apoptosis (TUNEL), and target engagement (tubulin polymerization status, H3K4me2 levels by immunohistochemistry). |
| ADME/Pharmacokinetics |
MY-943 is a small molecule with a molecular weight determined by its N-benzylarylamide-dithiocarbamate scaffold. For in vitro use, it is soluble in DMSO. For in vivo studies, it can be formulated in co-solvent systems such as 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline or in 0.5% methylcellulose for oral administration. Pharmacokinetic properties are not detailed in the literature.
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| Toxicity/Toxicokinetics |
MY-943 demonstrated no obvious toxicity at effective anti-tumor doses in the in situ gastric cancer mouse model. As a dual inhibitor of tubulin and LSD1, potential toxicities may include myelosuppression (due to tubulin inhibition in dividing hematopoietic cells) and epigenetic-related effects, but these have not been fully characterized.
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| References | |
| Additional Infomation |
MY-943 is a research-grade dual inhibitor for studying gastric cancer biology, tubulin dynamics, and LSD1-mediated epigenetic regulation. It has not been approved for clinical use. The compound acts on the colchicine binding site of beta-tubulin and modulates LSD1 activity. Molecular docking studies have explored its binding modes with both targets. This product is strictly for laboratory research.
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| Molecular Formula |
C30H36N4O6S2
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| Molecular Weight |
612.76
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| Appearance |
Light yellow to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1632 mL | 0.8160 mL | 1.6320 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.
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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