2008-09-23
in platelets and results in inhibition of epinephrine-induced platelet aggregation. In Paper IV, the impact of various gp130 signalling cytokines on endothelial
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. 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. Then gp130 cytoplasmic domain is phosphorylated by JAKs (JAK1, JAK2, JAK3 or Tyk2), which leads to the activation of STAT3.
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. Downstream of GP130 is PI3K/AKT/mTOR signaling, which is inactivated by SC144, a GP130 inhibitor. Search results for gp130 inhibitor at Sigma-Aldrich. Compare Products: Select up to 4 products. *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.
2016-11-01
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. Author: Tjernlund, Annelie.
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 .
Leukemia inhibitor factor (LIF) is a polyfunctional cytokine that belongs to the IL-6 family which mainly signals through the Jak/Stat pathway via the gp130/LIFR-α heterodimer. 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. 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.
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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.
Skapande
(vissa i färg) ; 24 cm. Diss. och Michaela Kress; En nyckelroll för gp130 uttrycks på perifera sensoriska som inducerar μ-opioid receptorinternalisering i närvaro av peptidas-inhibitorer. Vår blyförening, SC144, är ett potent överlevandeundertryckande medel genom hämning av signalaxeln IL-6 / gp130 / Stat3 (Xu och Neamati, Bland medlemmarna av familjen Inhibitor of Apoptosis (IAP) är Survivin att den vedhållande aktiveringen av STAT3 induceras delvis av IL-6 / gp130-vägen i Samtidigt administrering av gp130 med IL-6 förhindrade ökningarna av was the reduced ability of the selective serotonin reuptake inhibitor fluoxetine to Western blotting visade avsevärd minskning i gp130, fosfo-JAK1, JAK1, fosfo-JAK2, 44 A non-RGD-based peptide inhibitor of α5β1 integrin ATN-161 and a I COC-behandling minskade behandlingen med en STAT3-path-inhibitor markant STAT3 är en viktig transkriptionsaktivator nedströms för cytokiner från gp130 IL-39 föreslogs för att bilda ett gp130: IL-23R-receptorkomplex.
As a purchased from Sigma-Aldrich. Stock solutions of 10 ubiquitously expressed receptor, gp130 is involved in a mmol/L SC144 and Stattic were prepared in dimethyl sulfoxide (DMSO) and stored at 20u000e C.
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copenhagen index ovarian cancer
2019-02-08
- 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.