Referencia número: HY-149249

MY-943

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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 98.01%
No. CAS: 3043676-46-3
Fòrmula: C₃₀H₃₆N₄O₆S₂
Peso molecular:612.76

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MY-943 Chemical Structure

No. CAS: 3043676-46-3

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Histone Demethylase :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	253.9 nM Compound: I-25; MY-943	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
DU-145	IC₅₀	49.9 nM Compound: I-25; MY-943	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
ECa-109 cell line	IC₅₀	114.4 nM Compound: I-25; MY-943	Antiproliferative activity against human EC109 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human EC109 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
HCT-116	IC₅₀	0.044 μM Compound: I-25; MY-943	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
HGC-27	IC₅₀	24.5 nM Compound: I-25; MY-943	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
Huh-7	IC₅₀	47.9 nM Compound: I-25; MY-943	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
KYSE-450	IC₅₀	0.03 μM Compound: I-25; MY-943	Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
MCF7	IC₅₀	34.4 nM Compound: I-25; MY-943	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
MGC-803	IC₅₀	0.017 μM Compound: I-25; MY-943	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
NCI-H520	IC₅₀	22.5 nM Compound: I-25; MY-943	Antiproliferative activity against human NCI-H520 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human NCI-H520 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
PC-3	IC₅₀	44.6 nM Compound: I-25; MY-943	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
SGC-7901	IC₅₀	19.5 nM Compound: I-25; MY-943	Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
SMMC-7721	IC₅₀	27 nM Compound: I-25; MY-943	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]
TE-1	IC₅₀	31.4 nM Compound: I-25; MY-943	Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36940611]

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.

Chemical Information

No. CAS 3043676-46-3
Appearance Solid
Peso molecular 612.76
Fòrmula C₃₀H₃₆N₄O₆S₂
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Yuan XY, et al. Discovery of novel N-benzylarylamide-dithiocarbamate based derivatives as dual inhibitors of tubulin polymerization and LSD1 that inhibit gastric cancers. Eur J Med Chem. 2023 Apr 5;252:115281. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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MY-943

Ver todos los productos específicos de isoformas Histone Demethylase

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

MY-943 Related Classifications

HY-149249 Related Classifications

Bioz