In both cases, association with the signal transducing gp130 receptor is compulsory. However, differences in the downstream signaling mechanisms of IL-6

The IL-6 receptor blockers tocilizumab and sarilumab inhibit the low affinity IL-6 receptor to inhibit binding of IL-6 without interfering with binding to gp130 at

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. 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. 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.

For research use only. We do not sell to patients. SC144 hydrochloride Chemical Structure The shared receptor subunit designated glycoprotein 130 (gp130) is a receptor component for a variety of cytokines, including IL-6, IL-11, IL-27, IL-31, leukemia inhibitor factor (LIF), oncostatin M, ciliary neurotrophic factor, and cardiotropin-1. From a rheumatologist's perspective, IL-6 is the most important cytokine in this subfamily. small-molecule gp130 inhibitor with oral activity in ovar-ian cancer. Materials and Methods Reagents SC144, a quinoxalinhydrazide derivative, was synthe-sized as described (9). Stattic, a Stat3 inhibitor (12), was purchased from Sigma-Aldrich.

Jun 21, 2019 Sumanta Pal, MD:Beyond infigratinib, erdafitinib, and anti-FGFR3 [fibroblast growth factor receptor 3] monoclonal antibody B-701 vofatamab, gp130 Inhibitor, SC144.

2021-03-20

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.

gp130 Inhibitor, SC144 - Calbiochem Synonym: SC144, gp130 Inhibitor, SC144 - Calbiochem Empirical Formula (Hill Notation) C 16 H 11 FN 6 O · xHCl . Molecular Weight 322.30 (free base basis)

2017-07-03 · Interleukins-6 (IL-6)/GP130 signaling pathway represents a promising target for cancer therapy due to its critical role in survival and progression of multiple types of cancer. We have identified Bazedoxifene, a Food and Drug Administration (FDA)-approved drug used for the prevention of postmenopausal osteoporosis, with novel function as inhibitor of IL-6/GP130 interaction. In this study, we Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 infection.

Date: 2006-12-14. Location: Föreläsningssalen 4U Solen, Alfred Nobels Allé 8, Janus Kinase 2 Inhibitor AG490 Inhibits the STAT3 Signaling Pathway by Suppressing Protein Translation of gp130 In Ae Seo, 1 Hyun Kyoung Lee, 1 Yoon Kyung Shin, 1 Sang Hwa Lee, 2 Su-Yeong Seo, 2 Ji Wook Park, 3 and Hwan Tae Park 1 1 Department of Physiology, Medical Science Research Institute, College of Medicine, Dong-A University, Busan 602-714, Korea.: 2 Department of Microbiology, Medical gp130 Inhibitor, SC144 - Calbiochem Synonym: SC144, gp130 Inhibitor, SC144 - Calbiochem Empirical Formula (Hill Notation) C 16 H 11 FN 6 O · xHCl . Molecular Weight 322.30 (free base basis) 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.
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The inhibition of protein synthesis of gp130 by AG490 led to immediate loss of mature gp130 in cell membranes, due to its short half-life, thereby resulting in reduction in the STAT3 response to IL-6. Taken together, these results suggest that AG490 blocks the STAT3 activation pathway via a novel pathway. SC-144 is an orally active small-molecule gp130 inhibitor. Products are for laboratory research use only. Not for human use.

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.
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OPG inhibited 45Ca release stimulated by RANKL, hIL-6 plus shIL-6R, hLIF, hOSM, mOSM, and D3. An Ab neutralizing mouse gp130 inhibited 45Ca release

It can substantially increas Human colon cancer cells are sensitive to GP130 inhibition. 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.

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Inhibitor of gp130 (IC 50 = 0.72 μ M); blocks cytokine-triggered gp130 signaling. Induces gp130 phosphorylation and down regulates gp130 glycosylation; also abrogates STAT3 phosphorylation, nuclear translocation and inhibits the expression of downstream target genes. Delays tumor growth in a mouse xenograft model of human ovarian cancer

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. In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor.