NBDHEX

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NBDHEX 是谷胱甘肽 S-转移酶 P1-1 (GSTP1-1) 的有效抑制剂。

NBDHEX is a potent inhibitor of glutathione S-transferase P1-1 (GSTP1-1).(In Vitro):NBDHEX not only is cytotoxic toward the parental small cell lung cancer H69 cell line (LC(50) of 2.3 +/- 0.6 micromol/L) but also overcomes the multidrug resistance of its variant, H69AR, which overexpresses the ATP-binding cassette transporter multidrug resistance-associated protein 1 (MRP1;?LC(50) of 4.5 +/- 0.9 micromol/L).?Drug efflux experiments, done in the presence of a specific inhibitor of MRP1, confirmed that NBDHEX is not a substrate for this export pump .(In Vivo):NBDHEX, In female mice, treatment results in a statistically significant tumour inhibition (approximately 70%) .

Cell Viability Assay 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 (LC50 of 2.3 μM) and in its Adriamycin-resistant counterpart H69AR (LC50 of 4.5 μM).Apoptosis Analysis 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 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.

Animal Model:SCID female mice (4-5 weeks) injected with Me501 cells 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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Apoptosis

Apoptosis

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787634-60-0

297.33

C12H15N3O4S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (420.41 mM)

OCCCCCCSc1ccc([N+]([O-])=O)c2nonc12

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(-20℃)

With Ice Pack

≥ 2 years