Nur77 modulator 1

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

Nur77 调节剂 1 是一种良好的 Nur77 结合剂 (KD = 3.58 μM)。 Nur77 调节剂 1 上调 Nur77 表达，介导 Nur77 的亚细胞定位，诱导 Nur77 依赖性 ER 应激和自噬，并导致细胞凋亡。抗肝癌活性。

Nur77 modulator 1 is a good Nur77 binder (K D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .(In Vitro):Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line) . Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner . Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis . Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete) . Cell Viability Assay . Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Concentration: 0-20 μM. Incubation Time: 12-24 hours. Result: Exhibited IC 50 values of 0.6 μM, 0.89 μM, 1.40 μM and >20 μM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.(In Vivo):Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability . Animal Model: Nude mouse hepatoma HepG2 xenograft . Dosage: 10 and 20 mg/kg/day. Administration: IP, once every day for 15 days. Result: Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line).Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner.Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis.Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete). Cell Viability Assay.Cell Line:Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).Concentration:0-20 μM.Incubation Time:12-24 hours.Result:Exhibited IC50 values of 0.6 μM, 0.89 μM, 1.40 μM and >20 μM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively.Reduced the viability in a time-dependent manner.Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability. Animal Model:Nude mouse hepatoma HepG2 xenograft.Dosage:10 and 20 mg/kg/day.Administration:IP, once every day for 15 days.Result:Lead to substantial suppression of tumor growth.The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.Exhibited almost no influence on the body weight of experimental mice.

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Others

Other Targets

IGF-1R|Akt|mTOR

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2469975-55-9

495.6

C28H25N5O2S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (252.22 mM)

COC1=CC=CC2=C1N=C(C)C=C2NC3=CC=C(NC(C(N/N=C/C4=CC=C(SC)C=C4)=O)=C5)C5=C3

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(-20℃)

With Ice Pack

≥ 2 years