gp130 Inhibitor, SC144 - Calbiochem Cell-permeable inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells. Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. - Find MSDS or SDS, a COA, data sheets and more information.

Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 infection. Author: Tjernlund, Annelie. Date: 2006-12-14.

We do not sell to patients. Correction to: Bazedoxifene as a novel GP130 inhibitor for Colon Cancer therapy. Jia Wei Department of Hematology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, People's Republic of China. 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. It can substantially increas Human colon cancer cells are sensitive to GP130 inhibition.

Glucosamine-induced inhibition of N-glycosylation of gp130 represses the IL6/JAK/STAT3 signaling in DU145 cells. To determine whether the deficiency in N-glycosylation has any effects on the activity of the gp130-associated IL-6/JAK/STAT3 signaling [], we carried out the following investigations.First, we studied IL-6 binding to DU145 cells in the presence and absence of glucosamine. Repositioning Bazedoxifene as a novel IL-6/GP130 inhibitor for sarcoma therapy Lin, Jiayuh Nationwide Children's Hospital, Columbus, OH, United States Search 24 grants from Jiayuh Lin Search grants from Nationwide Children's Hospital. Share this grant: : Although inhibition of STAT3 phosphorylation roughly paralleled the time course of gp130 disappearance, inhibition of gp130 disappearance by caspase inhibitors did not restore IL‐6–mediated STAT3 activation in the presence of hydrophobic bile acids.

2014-09-30

Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. - Find MSDS or SDS, a COA, data sheets and more information. Soluble gp130 is the natural inhibitor of soluble interleukin-6 receptor transsignaling responses. 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.

Inhibitor of gp130 (IC50 = 0.72 μM); blocks cytokine-triggered gp130 signaling. Induces gp130 phosphorylation and down regulates gp130 glycosylation; also

2015-06-01 · Gp130 is the common β-receptor for all cytokines of the IL-6 family, including IL-6, IL-11, CLC, CNTF, CT-1, OSM, LIF and IL-27 [ 33 ]. Signal transduction is initiated after dimer formation with LIFR, OSMR, WSX-1 or gp130 itself. 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).

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. cancer cells, and that the inhibition of GP130 expression significantly reduces cell viability, survival and migration. Downstream of GP130 is PI3K/AKT/mTOR signaling, which is inactivated by SC144, a GP130 inhibitor. However, Raf/MEK/ERK signaling, which also is downstream of GP130 is activated by SC144. This 2019-02-08 · Bazedoxifene, a third- generation selective estrogen modulator approved by the Food and Drug Administration (FDA), is a novel inhibitor of IL-11/GP130 signaling discovered by docking modeling. 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.
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2009-04-30 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. It can substantially SC-144 is an orally active small-molecule gp130 inhibitor. Products are for laboratory research use only.

In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor.
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May 20, 2014 (OSM) or leukemia inhibitory factor (LIF). Such cytokines of the gp130 family may provide the redundancy important for myeloma cell growth.

Molecular Weight: 322.30 (free base basis) cancer cells, and that the inhibition of GP130 expression significantly reduces cell viability, survival and migration. Downstream of GP130 is PI3K/AKT/mTOR signaling, which is inactivated by SC144, a GP130 inhibitor.

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The binding of IL-6 to IL-6Rα induces trimer formation via recruitment of gp130 followed by formation of hexamer through homodimerization. Then gp130 cytoplasmic domain is phosphorylated by JAKs (JAK1, JAK2, JAK3 or Tyk2), which leads to the activation of STAT3. After phosphorylation, p-STAT3 serves a critical role as a transcription factor.

We do not sell to patients. SC144 hydrochloride Chemical Structure 2019-02-08 · Recently, using multiple-ligand simultaneous docking and drug repositioning, we identified bazedoxifene as a novel small-molecule inhibitor of GP130 . 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.

Although inhibition of STAT3 phosphorylation roughly paralleled the time course of gp130 disappearance, inhibition of gp130 disappearance by caspase inhibitors did not restore IL‐6–mediated STAT3 activation in the presence of hydrophobic bile acids.

Recombinant sgp130 protein could be used to block the anti‐apoptotic effect of sIL‐6R on lamina propria cells from Crohn disease patients. A wide range of bulk and speciality Glycoprotein 130 (gp130) inhibitors can be provided by BOC Sciences to the pharmaceutical, argochemical and biotechnology industries. 2015-06-01 · Gp130 is the common β-receptor for all cytokines of the IL-6 family, including IL-6, IL-11, CLC, CNTF, CT-1, OSM, LIF and IL-27 [ 33 ].

a: The expression of GP130, IL-11, IL-11Rα, IL-6, IL-6R, p-STAT3(Y705) and ER-α was evaluated in colon cancer cells. The first-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer (IC50 values 0.43-0.95 µM for a range of human ovarian cancer cell lines). SC144 binds gp130, induces gp130 phosphorylation and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. 2014-11-15 2017-07-01 One of these inhibitors, SC144, has been used to slow prostate, lung, breast, colorectal, and ovarian cancer progression and inhibit angiogenesis, in preclinical models (30, 64). SC144 is a small molecule inhibitor of gp130 and binds to S782 phosphorylated gp130, resulting in subsequent deglycosylation and inactivation of gp130 .