(-)-Xestospongin C - CAS 88903-69-9
Category: Inhibitor
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(-)-Xestospongin C is a potent and reversible inhibitor of IP3 receptor that reguates calcium release. (-)-Xestospongin C has been found to inhibit bradykinin-induced Ca2+ release in PC12 cells and attenuate PHP-induced IL-2 production in Jurkat T cells, but exhibits no effect on ryanodine receptor-mediated Ca2+ release in PC12 cells.
Brife Description:
IP3 receptor inhibitor
(1R,4aR,11R,12aS,13S,16aS,23R,24aS)-Eicosahydro-5H,17H-1,23:11,13-diethano-2H,14H-[1,11]dioxacycloeicosino[2,3-b:12,13-b']dipyridine; Xestospongin C
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1.Acetylcholine induces Ca2+ oscillations via m3/m4 muscarinic receptors in the mouse oocyte.
Kang D;Park JY;Han J;Bae IH;Yoon SY;Kang SS;Choi WS;Hong SG Pflugers Arch. 2003 Dec;447(3):321-7. Epub 2003 Oct 14.
Changes in intracellular Ca2+ concentration are required for the activation of mammalian oocytes. They are caused mainly by Ca2+ release from the endoplasmic reticulum (ER) via Ins P3 receptors (Ins P3R). Several studies have reported that acetylcholine (ACh) is capable of triggering early activation events in mouse oocytes over-expressed with the m1 muscarinic ACh receptor (m1AChR). Here we examined which subtypes of the mAChR (m1 to m4) are involved in the generation of Ca2+ oscillations in native mouse oocytes. ACh (10 microM) elicited regular Ca2+ oscillations similar to those induced by sperm in their temporal characteristics. The Ca2+ oscillations were abolished by application with atropine, the mAChR inhibitor. Within 1 min after treatment of ACh, intracellular Fluo-3 fluorescence intensity increased from 794+/-119 to 2023+/-755 (increase to 250% of original value), indicating a strong rise of cytosolic Ca2+ concentration. 4-DAMP mustard and Tropicamide, specific antagonists of m3AChR and m4AChR, completely abolished ACh-induced Ca2+ oscillations. In the ovulated oocytes, the expression of m3/m4 AChR was clearly detected by RT-PCR analysis. Furthermore, ACh-induced Ca2+ oscillations were also abolished or decreased by PLC inhibitors (U73122 or D609) and an Ins P3-receptor antagonist (xestospongin C), confirming that ACh generates Ca2+ oscillations via the PLC-Ins P3 (PI) pathway.
2.The presenilin 1 deltaE9 mutation gives enhanced basal phospholipase C activity and a resultant increase in intracellular calcium concentrations.
Cedazo-Minguez A;Popescu BO;Ankarcrona M;Nishimura T;Cowburn RF J Biol Chem. 2002 Sep 27;277(39):36646-55. Epub 2002 Jul 16.
We studied effects of the familial Alzheimer's disease presenilin 1 (PS1) exon 9 deletion (PS1-DeltaE9) mutation on basal and carbachol-stimulated phosphoinositide (PI) hydrolysis and intracellular Ca(2+) concentrations ([Ca(2+)](i)) in human SH-SY5Y neuroblastoma cells. We demonstrate that PS1-DeltaE9 cells have an enhanced basal PI hydrolysis and [Ca(2+)](i) as compared with both wild type PS1 (PS1-WT) and nontransfected (NT) cells. Both were reversed by the phospholipase C (PLC) inhibitor neomycin. The PS1-DeltaE9-related high basal [Ca(2+)](i) was also reversed by xestospongin C confirming that this effect was inositol trisphosphate receptor-mediated. Carbachol gave a greater stimulation of [Ca(2+)](i) in PS1-DeltaE9 cells that took longer to return to basal as compared with responses seen in NT and PS1-WT cells. This long tail-off effect seen in PS1-DeltaE9 cells after carbachol stimulation was reversed by xestospongin C and dantrolene, suggesting that it was mediated by inositol trisphosphate receptor and ryanodine receptor amplification of Ca(2+). Ruthenium red only reduced carbachol peak elevations of [Ca(2+)](i) in NT and PS1-WT cells and not in PS1-DeltaE9 cells. No significant between cell type differences were seen for basal and carbachol-stimulated [Ca(2+)](i) with either ryanodine or the endoplasmic reticulum Ca(2+) ATPase inhibitor cyclopiazonic acid.
3.Xestospongin C, a novel blocker of IP3 receptor, attenuates the increase in cytosolic calcium level and degranulation that is induced by antigen in RBL-2H3 mast cells.
Oka T;Sato K;Hori M;Ozaki H;Karaki H Br J Pharmacol. 2002 Apr;135(8):1959-66.
1. We evaluated the role of the cross-linking of Fc epsilon RI-mediated inositol 1,4,5-triphosphate (IP(3)) in the increase in cytosolic Ca(2+) level ([Ca(2+)](i)) using xestospongin C, a selective membrane permeable blocker of IP(3) receptor, in RBL-2H3 mast cells. 2. In the cells sensitized with anti-dinitrophenol (DNP) IgE, DNP-human serum albumin (DNP-HSA) and thapsigargin induced degranulation of beta-hexosaminidase and a sustained increase in [Ca(2+)](i). Xestospongin C (3 - 10 microM) inhibited both of these changes that were induced by DNP-HSA without changing those induced by thapsigargin. 3. In the absence of external Ca(2+), DNP-HSA induced a transient increase in [Ca(2+)](i). Xestospongin C (3 - 10 microM) inhibited this increase in [Ca(2+)](i). 4. In the cells permeabilized with beta-escin, the application of IP(3) decreased Ca(2+) in the endoplasmic reticulum (ER) as evaluated by mag-fura-2. Xestospongin C (3 - 10 microM) inhibited the effect of IP(3). 5. After the depletion of Ca(2+) stores due to stimulation with DNP-HSA or thapsigargin, the addition of Ca(2+) induced capacitative calcium entry (CCE). Xestospongin C (3 - 10 microM) inhibited the DNP-HSA-induced CCE, whereas it did not affect the thapsigargin-induced CCE.
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CAS 88903-69-9 (-)-Xestospongin C

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