| 中文名称 |
NBDHEX
|
| 英文名称 |
NBDHEX
|
| 英文别名 |
1-HEXANOL, 6-[(7-NITRO-2,1,3-BENZOXADIAZOL-4-YL)THIO]-;NBDHEX
|
| Cas No. |
787634-60-0
|
| 分子式 |
C12H15N3O4S
|
| 分子量 |
297.33
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
NBDHEX 是一种有效的谷胱甘肽 S-转移酶 P1-1 (GSTP1-1) 抑制剂。 NBDHEX 诱导肿瘤细胞凋亡。NBDHEX 通过抑制 GST 的催化活性,避免抑制剂被特异性泵从细胞中排出,以及破坏 GSTP1-1 和关键信号传导因子之间的相互作用,从而起到抗癌的作用。NBDHEX 也可以作为晚期自噬抑制剂。
|
| 产品详情 |
NBDHEX 是一种有效的谷胱甘肽 S-转移酶 P1-1 (GSTP1-1) 抑制剂。 NBDHEX 诱导肿瘤细胞凋亡。NBDHEX 通过抑制 GST 的催化活性,避免抑制剂被特异性泵从细胞中排出,以及破坏 GSTP1-1 和关键信号传导因子之间的相互作用,从而起到抗癌的作用。NBDHEX 也可以作为晚期自噬抑制剂。
|
| 生物活性 |
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
| 性状 |
Solid
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| IC50 & Target[1][2] |
Glutathione S-transferase P1-1 (GSTP1-1);
Apoptosis;
Autophagy
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| 体外研究(In Vitro) |
NBDHEX (0.05-20 μM; 48 hours; H69 and H69AR cells) is cytotoxic toward cell lung cancer H69 and H69AR cells.NBDHEX (0-5 μM; 24 hours; H69AR cells) treatment results in a dose-dependent apoptosis in the H69AR cell line.NBDHEX (3 μM; 1-12 hours; H69AR cells) treatment increases the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion.NBDHEX treatment shows a marked increase in phosphorylation of p38, and also increases GSSG content in a time-dependent manner in H69 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
NBDHEX (0.8-80 mg/kg/day; oral administration; daily; for 15 days; SCID female mice) treatment results a statistically significant tumour inhibition (approximately 70%). has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| 参考文献 |
[1]. Sha HH, et al. 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound. Biosci Rep. 2018 Feb 13;38(1). pii: BSR20171440.[2]. Filomeni G, et al. 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol, a specific glutathione S-transferase inhibitor, overcomes the multidrug resistance (MDR)-associated protein 1-mediated MDR in small cell lung cancer. Mol Cancer Ther. 2008 Feb;7(2):371-9
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| 溶解度数据 |
In Vitro: DMSO : 125 mg/mL (420.41 mM; Need ultrasonic)配制储备液
|
[1]. Sha HH, et al. 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound. Biosci Rep. 2018 Feb 13;38(1). pii: BSR20171440.[2]. Filomeni G, et al. 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol, a specific glutathione S-transferase inhibitor, overcomes the multidrug resistance (MDR)-associated protein 1-mediated MDR in small cell lung cancer. Mol Cancer Ther. 2008 Feb;7(2):371-9
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。