1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis Caspase Bcl-2 Family
  3. SP-6-27

SP-6-27 是一种结合于 β-微管蛋白的秋水仙碱位点的微管蛋白 (tubulin) 解聚剂。SP-6-27 在卵巢癌细胞中诱导 G2/M 期细胞周期阻滞。SP-6-27 通过上调 BaxApaf-1 caspase-6 caspase-9caspase-3 增强卵巢癌细胞的内在凋亡 (apoptosis) 。SP-6-27 降低卵巢癌细胞的迁移能力。SP-6-27 抑制人脐静脉内皮细胞的毛细血管管状结构形成。SP-6-27 对正常卵巢上皮细胞表现出最低的细胞毒性。当与 Cisplatin (HY-17394) 联合使用时,SP-6-27 在化疗敏感/耐药的卵巢癌细胞中表现出增强的细胞毒性。SP-6-27 可用于卵巢癌研究。

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SP-6-27

SP-6-27 Chemical Structure

CAS No. : 1384170-58-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer[1].

IC50 & Target

Bax

 

Caspase 3

 

Caspase-6

 

Caspase-9

 

体外研究
(In Vitro)

SP-6-27 (0.001-10 μM; 72 h) 在顺铂敏感和耐药的卵巢癌细胞中强力抑制增殖,并对正常 HOSEpiC 细胞表现出最低的细胞毒性 (OVCA 细胞的 IC50 为 0.10-0.84 μM,HOSEpiC 细胞为 83.35 μM)[1]
SP-6-27 (0.5 μM; 24 h) 扰乱 α-微管蛋白和 β-微管蛋白细胞骨架结构,降低卵巢癌细胞中的微管密度[1]
SP-6-27 (0.5 μM; 48 h) 降低卵巢癌细胞 (A2780) 的迁移能力[1]
SP-6-27 (0.5 μM; 24 h) 诱导顺铂敏感和耐药卵巢癌细胞的 G2-M 期细胞周期阻滞 [1]
SP-6-27 (0.5 μM; 24-48 h) 诱导顺铂敏感和耐药卵巢癌细胞凋亡[1].
SP-6-27 在卵巢癌细胞中上调促凋亡基因 (Bax、PAF-1、caspase-9、caspase-6、Caspase-3) 和 GADD45A[1]
SP-6-27 (0.5 μM; 24-48 h) 在与顺铂同时处理时增强顺铂敏感细胞的细胞毒性,并在顺铂耐药细胞中于顺铂处理后顺序处理时增强细胞毒性[1]
SP-6-27 (0.5-1 μM; 24 h) 抑制人脐静脉内皮细胞的毛细血管管状形成,即使在肿瘤条件培养基存在的情况下[1]

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

Cell Viability Assay[1]

Cell Line: cisplatin-sensitive OVCA (A2780, SKOV-3, TOV-112D), cisplatin-resistant OVCA (OVCAR-3, cis-A2780, cis-TOV-112D), HOSEpiC
Concentration: 0.001-10 μM
Incubation Time: 72 h
Result: Exhibited potent cytotoxicity against Cisplatin-sensitive OVCA cells with a mean IC50 of 0.14 μM and against cisplatin-resistant OVCA cells with a mean IC50 of 0.36 μM; showed minimal cytotoxicity with an IC50 of 83.35 μM in normal HOSEpiC cells.

Cell Migration Assay [1]

Cell Line: A2780 OVCA cells
Concentration: 0.5 μM
Incubation Time: 48 h
Result: Reduced migration compared to control cells when monitored over 48 h.

Cell Cycle Analysis[1]

Cell Line: Cisplatin-sensitive A2780 and Cisplatin-resistant cis-A2780 OVCA cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Caused a complete collapse of cells in G1 phase and a substantial increase in G2-M phase cells: 87.8% of A2780 cells were arrested in G2-M phase (vs. 16.40% in control) and 58.9% of cis-A2780 cells were arrested in G2-M phase (vs. 14.5% in control).

Apoptosis Analysis[1]

Cell Line: Cisplatin-sensitive A2780 and Cisplatin-resistant cis-A2780 OVCA cells
Concentration: 0.5 μM
Incubation Time: 24 h (caspase-3 microscopy); 24, 48 h (Annexin V/7-AAD)
Result: Caused a pronounced increase in Annexin-V positive cells (early/late apoptotic) in both cell types at 24 and 48 h; showed increased cleaved caspase-3 activity in A2780 cells compared to control cells.
分子量

384.48

Formula

C24H24N4O

CAS 号
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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SP-6-27
目录号:
HY-136893
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