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MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and suppressing cell migration, thus showing potential for use in gastric cancer research [1].
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50 mg | Inquiry | Backorder |
Description | MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and suppressing cell migration, thus showing potential for use in gastric cancer research [1]. |
In vitro | MY-943 exhibits antiproliferative activity against three cancer cell lines, with IC50 values of 0.019 μM for MGC-803 cells, 0.044 μM for HCT-116 cells, and 0.030 μM for KYSE450 cells [1]. It dose-dependently and time-dependently inhibits the viability of MGC-803 and SGC-7901 cells at concentrations of 10, 20, 30 nM over 20, 40, 48, 60 hours [1]. MY-943 (1, 5, 10 μM; 48 h) attenuates the alkylation of β-tubulin by EBI in a dose-dependent manner and prevents the formation of β-tubulin:EBI complex bands in MGC-803 and SGC-7901 cells [1]. Concentration-dependently, MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) inhibits tubulin polymerization in MGC-803 and SGC-7901 cells [1] and induces apoptosis in a dose-dependent manner [1]. The compound downregulates the expression of anti-apoptotic proteins Bcl-2 and Mcl-1 and upregulates cleaved Caspase-3 and Caspase-7 levels dose-dependently [1]. Additionally, MY-943 dose-dependently decreases the levels of Weel, CyclinB1, and CDC2 and increases the levels of phosphorylated histone H3, H3K4me1, and H3K4me2 [1]. It effectively induces G2/M phase arrest dose-dependently [1] and significantly inhibits the migratory capabilities of gastric cancer cells MGC-803 and SGC-7901 [1]. |
In vivo | MY-943 (25 mg/kg/day; intraperitoneal injection; 21 days) significantly inhibited the growth of gastric cancer in mice and substantially reduced the weight and volume of the mice's tumor tissues [1]. |
Molecular Weight | 612.76 |
Formula | C30H36N4O6S2 |
Storage | Shipping with blue ice. |
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