计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
NBDHEX
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
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 MAPK , and also increases GSSG content in a time-dependent manner in H69 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 (LC 50 of 2.3 μM) and in its Adriamycin-resistant counterpart H69AR (LC 50 of 4.5 μM). Apoptosis AnalysisCell 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 AnalysisCell 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.
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%). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID female mice (4-5 weeks) injected with Me501cellsDosage: 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.
IC50& Target:Glutathione S-transferase P1-1 (GSTP1-1), ,Apoptosis, ,Autophagy
规格
别名
北德意志交易所
规格或纯度
Moligand™,10mM in DMSO
英文名称
NBDHEX
生化机理
NBDHEX 是一种强效谷胱甘肽 S 转移酶 P1-1（GSTP1-1）抑制剂。NBDHEX 可诱导肿瘤细胞凋亡。NBDHEX 通过抑制谷胱甘肽 S 转移酶的催化活性来发挥抗癌作用，从而避免了抑制剂从细胞中排出的不便。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=C(C2=NON=C2C(=C1)SCCCCCCO)[N+](=O)[O-]
PubChem CID
MeSH Entry Terms
6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol;NBDHEX compound
分子量
297.33
技术文档
高级数据
关联靶点（人）
GSTP1
Tchem
谷胱甘肽S转移酶P(Glutathione S-transferase P)
(1 活性数据)
GSTM2
Tchem
谷胱甘肽S-转移酶Mu2(Glutathione S-transferase Mu 2)
(2 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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