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 potentglutathione S-transferase P1-1 (GSTP1-1)inhibitor. NBDHEX inducesapoptosisof tumor cells. NBDHEX acts as an anticancer agent by inhibitingGSTscatalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between theGSTP1-1and key signaling effectors. NBDHEX can also act as late-phaseautophagyinhibitor[1][2]. |
| IC50& Target | Glutathione S-transferase P1-1 (GSTP1-1)[1];
Apoptosis[1];
Autophagy[1] |
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[2].
NBDHEX (0-5 μM; 24 hours; H69AR cells) treatment results in a dose-dependent apoptosis in the H69AR cell line[2].
NBDHEX (3 μM; 1-12 hours; H69AR cells) treatment increases the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion[2].
NBDHEX treatment shows a marked increase in phosphorylation of p38MAPK, and also increases GSSG content in a time-dependent manner in H69 cells[2].
Cell Viability Assay[2] | Cell Line: | H69 and H69AR cells | | Concentration: | 0.05-20 μM | | Incubation Time: | 48 hours | | Result: | The dose-response profiles revealed a good cytotoxic activity both in sensitive H69 cell line (LC50of 2.3 μM) and in its Adriamycin-resistant counterpart H69AR (LC50of 4.5 μM). |
Apoptosis Analysis[2] | Cell Line: | H69AR cells | | Concentration: | 0 μM, 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM | | Incubation Time: | 24 hours | | Result: | Resulted in a dose-dependent apoptosis in the H69AR cell line. |
Western Blot Analysis[2] | Cell Line: | H69AR cells | | Concentration: | 3 μM | | Incubation Time: | 1 hour,3 hours, 6 hours, 12 hours | | Result: | Increased the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion. |
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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%)[2].
| Animal Model: | SCID female mice (4-5 weeks) injected with Me501cells[3] | | Dosage: | 0.8 mg/kg/day, 8.0 mg/kg/day or 80 mg/kg/day | | Administration: | Oral administration; daily; for 15 days | | Result: | A statistically significant tumour inhibition (approximately 70%) was observed. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(420.41 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.3633 mL | 16.8163 mL | 33.6327 mL | | 5 mM | 0.6727 mL | 3.3633 mL | 6.7265 mL | | 10 mM | 0.3363 mL | 1.6816 mL | 3.3633 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (7.00 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (7.00 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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