SPHINX
目录号 : GC65981SPHINX 是 SRPK1 的选择性抑制剂,IC50 值为 0.58 μM。SPHINX 有效地减少体内脉络膜新生血管 (CNV)。SPHINX 可用于老年性黄斑变性的研究。
Cas No.:848057-98-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.58 μM (SRPK1)[1]
SPHINX is a selective SRPK1 inhibitor with an IC50 value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD[1].
SPHINX (10 μM; 2 h) affects EGF-induced phosphorylation of SRSF1 and SRSF2[1].
SPHINX (5 μM; 24 h) reduces the expression of VEGF165 relative to GAPDH control either in primary RPE and ARPE-19 cell lines[1].
Western Blot Analysis[1]
Cell Line: | ARPE-19 cell line |
Concentration: | 10 μM |
Incubation Time: | 2 hours |
Result: | Blocked EGF-induced phosphorylation of SRSF1 and SRSF2. |
SPHINX (10 ng; i.o. on laser photocoagulation day 0 and day 7) affects neovascular growth in vivo[1].
SPHINX (25 ng; i.o. on laser photocoagulation day 0 and day 7) affects the CNV area in CNV rats[1].
Animal Model: | C57/B6 mice with laser-induced CNV[1] |
Dosage: | 10 ng |
Administration: | Intraocular injection; 10 ng on laser photocoagulation day 0 and day 7 |
Result: | Significantly reduced neovascular growth compared with saline-injected controls. |
Animal Model: | Norway Brown rats with laser-induced choroidal neovascularization[1] |
Dosage: | 25 ng (10 ng/uL) |
Administration: | Intraocular injection; 25 ng (10 ng/uL) on laser photocoagulation day 0 and day 7 |
Result: | Significantly reduced the CNV area compared with saline injected controls. |
Cas No. | 848057-98-7 | SDF | Download SDF |
分子式 | C17H17F3N2O3 | 分子量 | 354.32 |
溶解度 | DMSO : 50 mg/mL (141.12 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
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1 mM | 2.8223 mL | 14.1115 mL | 28.2231 mL |
5 mM | 0.5645 mL | 2.8223 mL | 5.6446 mL |
10 mM | 0.2822 mL | 1.4112 mL | 2.8223 mL |
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Meeting the SPHINX
Int J Psychoanal 2022 Dec;103(6):965-978.PMID:36533647DOI:10.1080/00207578.2022.2086057.
Here I present a close re-reading and creative expansion of Richard Rusbridger's (2004) clinical work with a patient who reported a dream of a hybrid woman. Building on W. R. Bion's reading of the Oedipus myth and Melanie Klein's theory of the combined parent figure, and drawing on imagery ancient and modern, I re-interpret the patient's dream as an encounter with the SPHINX. Why does this enigmatic figure, threatening annihilation, emerge at this particular threshold in the patient's analysis? To explore this question, I return to Sophocles' Oedipus the King and offer a new translation of the exchange between Tiresias and Oedipus as they debate the king's famous victory over the monster. Where (and when) do we meet the SPHINX today? What form does the ancient monster take in modern life? In this paper, I ask us to consider what it means to meet the Sphinx-and how we might respond.
Who moves the SPHINX? An overview of intracellular sphingolipid transport
Biochim Biophys Acta Mol Cell Biol Lipids 2021 Nov;1866(11):159021.PMID:34339859DOI:10.1016/j.bbalip.2021.159021.
Lipid bilayers function as boundaries that enclose their content from the surrounding media, and the composition of different membrane types is accurately and dynamically tailored so that they can perform their function. To achieve this balance, lipid biosynthetic machinery and lipid trafficking events are intertwined into an elegant network. In this review, we focus on the intracellular movement of sphingolipids mediated by sphingolipid transfer proteins. Additionally, we will focus on the best characterized and understood mammalian sphingolipid transfer proteins and provide an overview of how they are hypothesized to function. Some are already well understood, while others remain enigmatic. A few are actual lipid transfer proteins, moving lipids from membrane to membrane, while others may have more of a sensor role, possibly reacting to changes in the concentrations of their ligands. Considering the substrates available for cytosolic sphingolipid transfer proteins, one open question that is discussed is whether galactosylceramide is a target. Another question is the exact mechanics by which sphingolipid transfer proteins are targeted to different organelles, such as how four phosphate adapter protein-2, FAPP2 is targeted to the endoplasmic reticulum. The aim of this review is to discuss what is known within the field today and to provide a basic understanding of how these proteins may work.
Uncovering the 'SPHINX' of sphingosine 1-phosphate signalling: from cellular events to organ morphogenesis
Biol Rev Camb Philos Soc 2022 Feb;97(1):251-272.PMID:34585505DOI:10.1111/brv.12798.
Sphingosine 1-phosphate (S1P) is a bioactive sphingolipid metabolite, functioning as a signalling molecule in diverse cellular processes. Over the past few decades, studies of S1P signalling have revealed that the physiological activity of S1P largely depends on S1P metabolizing enzymes, transporters and receptors on the plasma membrane, as well as on the intracellular proteins that S1P binds directly to. In addition to its roles in cancer signalling, immunity and inflammation, a large body of evidence has identified a close link of S1P signalling with organ morphogenesis. Here we discuss the vital role of S1P signalling in orchestrating various cellular events during organ morphogenesis through analysing each component along the extracellular and intracellular S1P signalling axes. For each component, we review advances in our understanding of S1P signalling and function from the upstream regulators to the downstream effectors and from cellular behaviours to tissue organization, primarily in the context of morphogenetic mechanisms. S1P-mediated vesicular trafficking is also discussed as a function independent of its signalling function. A picture emerges that reveals a multifaceted role of S1P-dependent pathways in the development and maintenance of organ structure and function.
Riddle of the SPHINX: Emerging Role of Transfer RNAs in Human Cancer
Front Pharmacol 2021 Dec 15;12:794986.PMID:34975491DOI:10.3389/fphar.2021.794986.
The dysregulation of transfer RNA (tRNA) expression contributes to the diversity of proteomics, heterogeneity of cell populations, and instability of the genome, which may be related to human cancer susceptibility. However, the relationship between tRNA dysregulation and cancer susceptibility remains elusive because the landscape of cancer-associated tRNAs has not been portrayed yet. Furthermore, the molecular mechanisms of tRNAs involved in tumorigenesis and cancer progression have not been systematically understood. In this review, we detail current knowledge of cancer-related tRNAs and comprehensively summarize the basic characteristics and functions of these tRNAs, with a special focus on their role and involvement in human cancer. This review bridges the gap between tRNAs and cancer and broadens our understanding of their relationship, thus providing new insights and strategies to improve the potential clinical applications of tRNAs for cancer diagnosis and therapy.
The SPHINX's riddle: cardiovascular involvement in autoimmune rheumatic disease
BMC Cardiovasc Disord 2016 Oct 28;16(1):204.PMID:27793103DOI:10.1186/s12872-016-0381-5.
Factors leading to Cardiovascular Disease (CVD) in Autoimmune Rheumatic Diseases (ARD) include: a) atherosclerosis and macro-microvascular coronary artery disease b) pericardial, myocardial and vascular inflammation c) heart valve disease d) heart failure and e) pulmonary hypertension.Cardiology utilizes various non-invasive imaging modalities, such as rest/stress Electrocardiogram (ECG), echocardiography, nuclear imaging and more recently Cardiovascular Magnetic Resonance (CMR) to detect ischemic or inflammatory disease in ARD. Exercise ECG is a reliable prognostic test for identification of patients either very unlikely or very likely to have cardiac events. However, this is not the case for intermediate risk patients. In stress echocardiography the diagnostic end point for the detection of myocardial ischemia is the induction of a transient worsening in regional function during stress. It provides similar diagnostic and prognostic accuracy as radionuclide stress perfusion, but at a lower cost and without radiation exposure. Stress Myocardial Perfusion Scintigraphy (MPS) is a non-invasive imaging modality for patients with suspected coronary artery disease, but has important limitations including radiation exposure, imaging artefacts and low spatial resolution, which preclude detection of small myocardial scars commonly found in ARD. By identifying early stages of inflammation and perfusion defects, CMR can shed light on the exact pathophysiologic background of myocardial lesions, even if the underlying ARD seems stable. However, high cost and lack of availability and expertise limit wider adoption.Hopefully, CMR will not have the same fate as Oedipous, who despite answering the SPHINX's riddle successfully, finally came to a bitter end; for in the case of CMR overcoming fate is, in fact, in our hands.