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  3. Avicin G

Avicin G 是一种鞘磷脂酶抑制剂和质膜破坏剂。Avicin G 可抑制中性鞘磷脂酶 (SMPD2/3) 和酸性鞘磷脂酶 (SMPD1) 的酶活性,提升细胞内鞘磷脂水平,并改变鞘磷脂的分布。Avicin G 会干扰结合 GTP 和 GDP 的 H-Ras 的侧向分离,抑制致癌性 K-和 H-Ras 的信号输出,减少 ERKAkt 的磷酸化,升高溶酶体 pH 值,并抑制表皮生长因子受体的内吞循环。Avicin G 可用于胰腺导管腺癌、非小细胞肺癌的相关研究。

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Avicin G

Avicin G Chemical Structure

CAS No. : 197787-17-0

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  • 生物活性

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  • 参考文献

生物活性

Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer[1].

体外研究
(In Vitro)

Avicin G (50-500 nM; 48 h) 可在 MDCK 细胞中使 mGFP-K-RasG12V 从质膜错误定位至内膜系统,处理 48 h 后的 IC50 为 73.8 nM[1]
Avicin G (500 nM; 48 h) 可在 MDCK 细胞中使 mGFP-K-RasG12V 从质膜转运至多种内膜区室,包括早期内体、晚期内体、溶酶体、线粒体、高尔基体和内质网,同时增加 LAMP1 阳性囊泡的数量和大小[1]
Avicin G (5-500 nM; 48 h) 可通过降低表达 mGFP-K-RasG12V 或 mGFP-H-RasG12V 的 MDCK 细胞中磷酸化 ERKAkt 的水平,抑制致癌性 Ras 信号输出,并上调 mGFP-K-RasG12V 的表达水平[1]
Avicin G (1.25 μM; 4 days with daily media replacement) 可抑制 KRAS 依赖型人胰腺导管腺癌 (PDAC) 和非小细胞肺癌 (NSCLC) 细胞系的生长[1]
Avicin G (500 nM; 48 h) 可破坏 BHK 细胞中 mGFP-K-RasG12V 的质膜纳米簇结构,以及 GTP 结合型与 GDP 结合型 mGFP-H-RasG12V 的侧向分离,从而导致致癌性 Ras 信号输出降低[1]
Avicin G (5-1000 nM; 48 h) 可在表达 mGFP-K-RasG12V 的 MDCK 细胞中抑制中性鞘磷脂酶活性,且其效力高于对酸性鞘磷脂酶活性的抑制;处理 48 h 后,在≥5 nM 浓度下对中性 SMase 产生显著抑制,在≥500 nM 浓度下对酸性 SMase 产生显著抑制[1]
Avicin G (5-1000 nM; 48 h) 会破坏 MDCK 细胞中 SMPD1-GFP 和 SMPD2-GFP 的亚细胞定位;在浓度≥500 nM 时降低 SMPD1-GFP 的表达量,在浓度≥10 nM 时升高 SMPD2-GFP 的表达量,且对 SMPD3-GFP 的表达及定位无影响[1]
Avicin G (10-1000 nM; 48 h) 以剂量依赖的方式升高 WT MDCK 细胞中的溶酶体 pH,在高浓度处理 48 h 后可将 pH 从 3.7 显著提升至 5.7[1]
Avicin G (100 nM; 48 h, with continued presence during subsequent serum starvation and EGF treatment) 可抑制 CHO 细胞中 EGFR-mGFP 的内吞循环,导致 EGFR-mGFP 在核周区域积累,而非返回质膜[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MDCK cells stably expressing mGFP-K-RasG12V or mGFP-H-RasG12V
Concentration: 5 nM, 10 nM, 100 nM, 500 nM
Incubation Time: 48 h
Result: Significantly reduced ppERK and pAkt levels in both K-RasG12V and H-RasG12V cells, with greater effects observed in K-RasG12V cells.
Significantly increased the expression level of mGFP-K-RasG12V, but not mGFP-H-RasG12V.

Cell Proliferation Assay[1]

Cell Line: Human pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC) cells
Concentration: 1.25 μM
Incubation Time: 4 days, with daily media replacement
Result: Significantly inhibited the growth of all tested K-Ras-addicted PDAC cell lines (AsPC-1, Panc10.05, MiaPaCa-2, HPAF-II, PANC-1) and K-Ras-addicted NSCLC cell lines (H358, H441).

Western Blot Analysis[1]

Cell Line: MDCK cells stably expressing SMPD1-GFP, SMPD2-GFP, or SMPD3-GFP
Concentration: 5 nM, 10 nM, 100 nM, 500 nM, 1000 nM
Incubation Time: 48 h
Result: Disrupted the lysosomal localization of SMPD1-GFP and accumulated SMPD2-GFP in vesicular structures, but did not alter the PM localization of SMPD3-GFP.
Significantly reduced SMPD1-GFP expression at ≥500 nM.
Significantly increased SMPD2-GFP expression at ≥10 nM.
Did not change SMPD3-GFP expression.
分子量

2067.26

Formula

C98H155NO45

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Avicin G
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HY-134505
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