NBDHEX

小分子

北德意志交易所

NBDHEX

N655369-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

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

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。

787634-60-0(DMSO)

C12H15N3O4S

297.33 g/mol

C1=C(C2=NON=C2C(=C1)SCCCCCCO)[N+](=O)[O-]