gp130 Inhibitor, SC144-Calbiochem

产品说明

一般描述

A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC₅₀ = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC₅₀ = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).

生化/生理作用

Primary Target
gp130

警告

Toxicity: Standard Handling (A)

其他说明

Xu, S., et al. 2013. Mol. Cancer Ther.12, 937.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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