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MY-943

CAS No. :

MCE 站：MY-943

产品活性：MY-943 是一种有效的 tubulin polymerization 和 LSD1 抑制剂，具有抗癌活性。 MY-943 诱导 G2/M 期阻滞和细胞凋亡，并抑制细胞迁移，可用于胃癌的研究。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis  |  Epigenetics

作用靶点：Microtubule/Tubulin  |  Apoptosis  |  Histone Demethylase

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.
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.
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.
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) concentration-dependently inhibits tubulin polymerization in MGC-803 ａnd SGC-7901 cells.
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) dose-dependently induces cell apoptosis.
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.
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.
MY-943 (10, 20, 30 nM; 8, 16, 24 nM; 48 h) effectively ａnd dose-dependently induces G2/M phase arrest.
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.

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.

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