SC144 hydrochloride |
| رقم الكتالوجGC37603 |
هيدروكلوريد SC144 هو مثبط gp130 النشط عن طريق الفم (IL6-beta) الأول في فئتهيربط هيدروكلوريد SC144 gp130 ، ويحفز الفسفرة gp130 (S782) وإزالة الجليكوزيل ، ويلغي فسفرة Stat3 والانتقال النووي ، ويمنع أيضًا التعبير عن الجينات المستهدفة النهائيةيُظهر هيدروكلوريد SC144 تثبيطًا قويًا للإشارات التي تسببها يجند gp130هيدروكلوريد SC144 يستحث موت الخلايا المبرمج في خلايا سرطان المبيض البشرية
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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