SC144 hydrochloride |
| Katalog-Nr.GC37603 |
SC144-Hydrochlorid ist ein erstklassiger, oral aktiver gp130 (IL6-beta)-Inhibitor. SC144-Hydrochlorid bindet gp130, induziert die gp130-Phosphorylierung (S782) und Deglykosylierung, hebt die Stat3-Phosphorylierung und Kerntranslokation auf und hemmt weiter die Expression nachgeschalteter Zielgene. SC144-Hydrochlorid zeigt eine starke Hemmung der durch den gp130-Liganden ausgelÖsten SignalÜbertragung. SC144-Hydrochlorid induziert Apoptose in menschlichen Eierstockkrebszellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 917497-70-2
Sample solution is provided at 25 µL, 10mM.
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SC144 hydrochloride is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.
[1]. Xu S, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.
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