SC144 hydrochloride |
| Catalog No.GC37603 |
El clorhidrato SC144 es el primer inhibidor de gp130 (IL6-beta) activo por vÍa oral de primera clase. El clorhidrato de SC144 se une a gp130, induce la fosforilaciÓn de gp130 (S782) y la desglicosilaciÓn, anula la fosforilaciÓn de Stat3 y la translocaciÓn nuclear, e inhibe aÚn mÁs la expresiÓn de los genes diana aguas abajo. El clorhidrato SC144 muestra una potente inhibiciÓn de la seÑalizaciÓn activada por el ligando gp130. El clorhidrato de SC144 induce la apoptosis en células de cÁncer de ovario humano.
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.
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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