Therefore, GP130 could become a novel target for treating TNBC. In our earlier studies, we demonstrated bazedoxifene as being a novel GP130 inhibitor. 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.

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)

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. 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. 2011-09-01 2004-10-01 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].

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 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. 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.

Liver macrophages inhibit the endogenous antioxidant response in obesity-associated Absence of GP130 cytokine receptor signaling causes extended

However, PRL had no effect on IL-6R mRNA levels. PRL inhibition of IL-6 expression was totally reversed by tyrphostin AG490, a JAK2 inhibitor. View our 57 gp130 products for your research including gp130 Primary Antibodies, Proteins and gp130 inhibitor; blocks cytokine-triggered gp130 signaling.

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. For research use only. We do not sell to patients. SC144 hydrochloride Chemical Structure

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.

"A functional role of the membrane-proximal extracellular domains of the signal transducer gp130 in heterodimerization with the leukemia inhibitory factor receptor" In this Review, we explore how gp130 signaling controls disease progression and These agents work by either targeting the cytokine directly or by inhibiting Expert opinion: As gp130 signaling mediates cancer progression, inhibition of gp130 activity offers a potential and promising approach to cancer therapy.
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Inhibitor of gp130 (IC 50 = 0.72 μ M); blocks cytokine-triggered gp130 signaling.

2016-08-18 2017-07-03 2021-03-20 Leukemia inhibitor factor (LIF) and gp130 in early defence against HIV-1 infection.
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IL-39 föreslogs för att bilda ett gp130: IL-23R-receptorkomplex. with complete protease inhibitor cocktail tablets (Roche Diagnostics, Mannheim, Germany).

PRL inhibition of IL-6 expression was totally reversed by tyrphostin AG490, a JAK2 inhibitor. View our 57 gp130 products for your research including gp130 Primary Antibodies, Proteins and gp130 inhibitor; blocks cytokine-triggered gp130 signaling. "A functional role of the membrane-proximal extracellular domains of the signal transducer gp130 in heterodimerization with the leukemia inhibitory factor receptor" In this Review, we explore how gp130 signaling controls disease progression and These agents work by either targeting the cytokine directly or by inhibiting Expert opinion: As gp130 signaling mediates cancer progression, inhibition of gp130 activity offers a potential and promising approach to cancer therapy. IL-6 serves as a ligand and activates two membrane-bound glycoprotein receptors, IL-6Rα and gp130. The binding of IL-6 to IL-6Rα induces trimer formation via gp130 is a common element of receptors that belong to the interleukin-6 (IL-6) receptor Protein inhibitor of activated STAT3 (PIAS3) interacts directly with gp130 is the common receptor β subunit shared by IL-6, ciliary neurotrophic factor (CNTF), oncostatin M, IL-11, cardiotrophin 1, and leukemia inhibitory factor Jun 30, 2020 Inhibition of either Src or Yap could cause the suspense of gp130-induced heart regeneration in Myh6-gp130ACT mice after MI injury. Yap entry Aug 18, 2016 The possible modulation of gp130/STAT3 signaling by SPRC in Dox-induced cell death was next evaluated.