SC-144 is an orally active small-molecule gp130 inhibitor. Products are for laboratory research use only. Not for human use. We do not sell to patients.

SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3

Not for human use. We do not sell to patients. SC144 is an inhibitor of gp130 with IC50 values of 0.43 μmol/L and 0.88 μmol/L in NCI/ADR-RES and HEY cell lines, respectively [1]. SC144 is a ﬁrst-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer.

Gp130 inhibitor

Our previous work has repositioned this drug as a potent GP130 inhibitor in pancreatic cancer therapy , but its effects on colon Our results, therefore, support the idea that Bazedoxifene is a potent inhibitor of GP130, which is consistent with suppression of GP130 inhibits STAT3 activity and induces cell apoptosis . Bazedoxifene also inhibits pancreatic cancer cell migration. 2021-03-02 · Olamkicept comprises two gp130 extracellular domains dimerized by the Fc part of human IgG1 (sgp130Fc) in order to trap the complex of IL-6 and soluble IL-6R. This leads to inhibition of trans- signaling mainly affecting IL-6-driven chronic inflammation12. We introduced stabilizing modifications (EP1873166B1) into the initial version of sgp130Fc.

Material Safety Data Sheet or SDS for gp130 Inhibitor, SC144 - Calbiochem 506387 from MilliporeSigma for download or viewing in the browser.

Currently, there are no small-molecule inhibitors of gp130 under clinical development. In this study, we show that gp130 is an attractive drug target in ovarian cancer due to its role in promoting cancer progression via the activation of its downstream Stat3 signaling.

Signal transduction in response to interleukin-6 (IL-6) requires binding of the cytokine to its receptor (IL-6R) and subsequent homodimerization of the signal transducer gp130. In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor. Methods: In the current report, anti-tumor effect of bazedoxifene on TNBC was further evaluated in TNBC cell lines SUM159, MDA-MB-231, and MDA-MB-468.

Thus, inhibition of gp130 signaling results in an anticoagulant phenotype in these cells. Tissue factor regulation was further studied. Cell surface tissue factor protein was down-regulated 10-fold in MDA-MB-231 DN gp130 cells compared to MDA-MB-231 control cells.

In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor. Methods: In the current report, anti-tumor effect of bazedoxifene on TNBC was further evaluated in TNBC cell lines SUM159, MDA-MB-231, and MDA-MB-468. Currently, there are no small-molecule inhibitors of gp130 under clinical development. In this study, we show that gp130 is an attractive drug target in ovarian cancer due to its role in promoting cancer progression via the activation of its downstream Stat3 signaling. In the present study, we demonstrate that GP130 is over-expressed in cisplatin and gemcitabine-resistant bladder cancer cells, and that the inhibition of GP130 expression significantly reduces cell viability, survival and migration.

Similar to inhibition of gp130-Jak-Stat3 signaling, heterozygous knockout of Bmi-1 in Apc-mutant mice reduced tumor growth and increased the abundance of the cell cycle inhibitors p16 (also known as Ink4a and encoded by Cdkn2a) and p21 (also known as Waf1 or Cip1 and encoded by Cdkn1a). Here, Gp130 is part of the receptor signaling complexes for we show that the lead compound, SC144, is a ﬁrst-in-class at least 8 cytokines [interleukin (IL)-6, IL-11, IL-27, LIF, small-molecule gp130 inhibitor with oral activity in ovar- CNTF, OSM, CT-1, and CLC; ref. (3)].
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However, Raf/MEK/ERK signaling, which also is downstream of … 2019-02-08 2013-06-01 2019-11-01 2021-03-02 SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. Inhibition of gp130 dependent proliferation of BAF/3 cells. It was of interest to know whether sgp130 proteins interfered with the biological activity of IL‐6 and sIL‐6R.

SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. Selleck's SC144 has been cited by 6 publications Exp Ther Med, 2021, 21 (2):163 The binding of IL-6 to IL-6Rα induces trimer formation via recruitment of gp130 followed by formation of hexamer through homodimerization.
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SC-144 is an orally active small-molecule gp130 inhibitor. Products are for laboratory research use only. Not for human use. We do not sell to patients.

*Please select more than one item to compare Currently, there are no small-molecule inhibitors of gp130 under clinical development. In this study, we show that gp130 is an attractive drug target in ovarian cancer due to its role in promoting cancer progression via the activation of its downstream Stat3 signaling.