SMYD3-IN-2 是一种SMYD3抑制剂,可通过诱导致死性自噬来对抗胃癌。SMYD3-IN-2 对 SMYD3 和 BGC823 细胞具有抑制作用,IC50值分别为 0.81 μM 和 0.75 μM。SMYD3-IN-2 可用于癌症的研究。
生物活性 | SMYD3-IN-2 is aSMYD3inhibitor against gastriccancervia inducing lethalautophagy. SMYD3-IN-2 has inhibitory forSMYD3and BGC823 cells withIC50values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research ofcancer[1]. |
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体外研究 (In Vitro) | SMYD3-IN-2 (compound 7r) (1.0 μM) 对 SMYD3 和 BGC823 细胞表现出强效抑制能力,IC50值分别为 0.81 μM和 0.75 μM[1]. SMYD3-IN-2 (1.0 μM; 24 h) 可抑制 SMYD3 引起的 Akt 甲基化和激活[1]。 SMYD3-IN-2 (0-48 h) 通过诱导自噬性细胞死亡抑制 BGC823 胃腺癌细胞的增殖[1]。
Western Blot Analysis[1] Cell Line: | BGC823 cells | Concentration: | 1.0 μM | Incubation Time: | 24 h | Result: | Suppressed the methylation levels of H3K4 and could significantly inhibit the lysine methylation of Akt1 by SMYD3. |
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体内研究 (In Vivo) | SMYD3-IN-2 (compound 7r) (i.p.; 15 and 30 mg/kg) suppresses the growth of BGC823 xenograft models in vivo[1].
Animal Model: | Xenograft Balb/c nude mice models[1] | Dosage: | 15 and 30 mg/kg | Administration: | Intraperitoneally administration | Result: | Remarkably suppressed the tumor volume, tumor weight and growth curves of gastric cancer xenografts in a dose-dependent manner. Resulted in strong immunohistochemistry staining of LC3-II and p62, weak staining of p-Akt (T308) and Ki67. |
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储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |