Feb 8, 2019 The FDA-approved drug bazedoxifene, known as a selective estrogen modulator, is currently used for the postmenopausal osteoporosis [23].

Nov 22, 2017 We also compared the inhibitory effects of bazedoxifene with those of the GP130 inhibitor, SC144 and the STAT3 inhibitor, BP-1-102 on IL-6

2011-09-01 · To mechanistically link the control of disease processes with IL-6/STAT3 signaling, an increasing number of studies have used a gp130 knockin mouse model in which an amino acid substitution prevents feedback inhibition of the receptor, resulting in exaggerated STAT3 signaling (79, 98, 99). small-molecule inhibitor of GP130 [24]. Our previous work has repositioned this drug as a potent GP130 in-hibitor in pancreatic cancer therapy [25], but its effects on colon cancer have not been investigated. Although IL-6 has been associated with many epithelial cancers, IL-11 acts as a more potent driver of colorectal cancers [22]. Therefore, GP130 could become a novel target for treating TNBC.

Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. 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. 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. gp130 Inhibitor, SC144 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents. In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor.

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.

2011-09-01

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 ]. Signal transduction is initiated after dimer formation with LIFR, OSMR, WSX-1 or gp130 itself.

Interestingly, the soluble form of gp130 (sgp130) acts as a natural inhibitor of IL-6 signaling . The complex of (IL-6/sIL-6R)/sgp130 also inhibits IL-6 activity and limits systemic responses to IL-6, suggesting its importance in regulating IL-6 signaling and as a potential therapeutic agent in RA (10, 13).

Chemical Therapeutics Discovery of a Novel Orally Active Small-Molecule gp130 Inhibitor for the Treatment of Ovarian Cancer Shili Xu1, Fedora Grande1,2, Antonio Garofalo2, and Nouri Neamati1 Abstract Interleukin (IL)-6 andStat3 play key roles in ovarian cancer progression. 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.

Synonym: gp130 Inhibitor, SC144 - Calbiochem Empirical Formula (Hill Notation): C 16 H 11 FN 6 O · xHCl. 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. 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.
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Glycoprotein 130 (also known as gp130, IL6ST, IL6-beta or CD130) is a transmembrane protein which is the founding member of the class of all cytokine receptors. It forms one subunit of the type I cytokine receptor within the IL-6 receptor family. 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.

In this study, we Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 infection. Author: Tjernlund, Annelie.
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av A Krona · 2006 · Citerat av 1 — The function of OSM are unclear with conflicting reports of growth stimulatory or inhibitory effects in various cell types. OSM is known to signal through gp130

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 ]. 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).

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2011-09-01

SC144 is a ﬁrst-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer. 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 . 2019-02-08 · In conclusion, our results indicate that FDA-approved bazedoxifene, as a novel GP130 inhibitor that blocks IL-11 signaling and can be repurposed for the treatment of colon cancer. Combined bazedoxifene and oxaliplatin therapy may be a viable therapeutic approach for human colon cancer. Predictably, JAK1/2 inhibitors, such as AZD1480, impair GP130 signaling, and reduce colitis-associated colon and inflammation-associated GC development in mice . We have shown that this occurs through inhibition of STAT3 signaling in the epithelium ( 69 ), while others found that AZD1480 also reduced the abundance of tumor-associated myeloid cells and tumor angiogenesis ( 70 ).

TPX-0131 is a next-generation ALK inhibitor entering IND-enabling studies. has shown preclinical potent inhibition of wildtype and numerous ALK mutations,

The focus of my research has been to investigate and understand if and how LIF exerts HIV-1 suppressing activity. We correlate post-treatment induction of this pathway in anti-TNF non-responders and demonstrate in vivo amelioration of the activated myeloid-stromal niche, using a specific gp130 inhibitor 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.

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. 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.