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SYP-5 Sale

目录号 : GC32876

A HIF-1 inhibitor

SYP-5 Chemical Structure

Cas No.:1384268-04-5

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10mM (in 1mL DMSO)
¥894.00
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5mg
¥813.00
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10mg
¥1,428.00
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50mg
¥6,158.00
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100mg
¥10,710.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

The cells (1×105 cells/mL) are seeded into 96-well culture plates. After overnight ncubation, the cells are treated with various concentrations of SYP-5 (2, 10, 50 μM) for 24 h. Then 10μLMTT) solution (2.5 mg/mL in PBS) is added to each well, and the plates are incubated for additional 4 h at 37°C. After centrifugation (2500 rpm, 10 min), the medium containing MTT is aspirated, and 100 μL DMSO is added. The optical density of each well is measured at 570 nm with a SpectraMax Paradigm Reader[1].

References:

[1]. Wang LH, et al. SYP-5, a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis. Eur J Pharmacol. 2016 Nov 15;791:560-568.

产品描述

SYP-5 is an inhibitor of hypoxia-inducible factor-1 (HIF-1).1 It inhibits HIF-1 activity in a reporter assay when used at concentrations ranging from 0.1 to 100 ?M. SYP-5 (2, 10, and 50 ?M) reduces hypoxia- or VEGF-induced capillary tube formation in human umbilical vein endothelial cells (HUVECs). It inhibits the migration and invasion of Hep3B hepatocellular carcinoma and BCaP-37 breast cancer cells in a concentration-dependent manner.

1.Wang, L.-H., Jiang, X.-R., Yang, J.-Y., et al.SYP-5, a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesisEur. J. Pharmacol.791560-568(2016)

Chemical Properties

Cas No. 1384268-04-5 SDF
Canonical SMILES O=C(C1=C(O)C(C=CC(C)(C)O2)=C2C=C1)/C=C/C3=CC=CS3
分子式 C18H16O3S 分子量 312.38
溶解度 DMSO : 33.33 mg/mL (106.70 mM) 储存条件 Store at -20°C
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1 mM 3.2012 mL 16.0061 mL 32.0123 mL
5 mM 0.6402 mL 3.2012 mL 6.4025 mL
10 mM 0.3201 mL 1.6006 mL 3.2012 mL
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Research Update

SYP-5 regulates meiotic thermotolerance in Caenorhabditis elegans

J Mol Cell Biol 2021 Dec 6;13(9):662-675.PMID:34081106DOI:10.1093/jmcb/mjab035.

Meiosis produces the haploid gametes required by all sexually reproducing organisms, occurring in specific temperature ranges in different organisms. However, how meiotic thermotolerance is regulated remains largely unknown. Using the model organism Caenorhabditis elegans, here, we identified the synaptonemal complex (SC) protein SYP-5 as a critical regulator of meiotic thermotolerance. syp-5-null mutants maintained a high percentage of viable progeny at 20°C but produced significantly fewer viable progeny at 25°C, a permissive temperature in wild-type worms. Cytological analysis of meiotic events in the mutants revealed that while SC assembly and disassembly, as well as DNA double-strand break repair kinetics, were not affected by the elevated temperature, crossover designation, and bivalent formation were significantly affected. More severe homolog segregation errors were also observed at elevated temperature. A temperature switching assay revealed that late meiotic prophase events were not temperature-sensitive and that meiotic defects during pachytene stage were responsible for the reduced viability of SYP-5 mutants at the elevated temperature. Moreover, SC polycomplex formation and hexanediol sensitivity analysis suggested that SYP-5 was required for the normal properties of the SC, and charge-interacting elements in SC components were involved in regulating meiotic thermotolerance. Together, these findings provide a novel molecular mechanism for meiotic thermotolerance regulation.

SYP-5, a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis

Eur J Pharmacol 2016 Nov 15;791:560-568.PMID:27664769DOI:10.1016/j.ejphar.2016.09.027.

Hypoxia-inducible factor-1 (HIF-1) plays an essential role in carcinogenesis. The overexpression of HIF-1 induced by hypoxia is closely associated with metastasis, poor prognosis and high mortality. In this study, a novel HIF-1 inhibitor SYP-5 was first observed by the luciferase reporter assay. Western blots results showed SYP-5 inhibited hypoxia-induced upregulation of HIF-1. Moreover, the proteins of vascular endothelial growth factor (VEGF) and matrix metalloproteinases (MMP)-2 that are targets of HIF-1, were down-regulated by SYP-5. Furthermore, in the tube formation assay, SYP-5 suppressed angiogenesis induced by hypoxia and VEGF in vitro. Additionally, using Transwell and RTCA assays, we found that SYP-5 also retarded the Hep3B and Bcap37 cells migration and invasion induced by hypoxia and FBS. Last, we also detected the upstream pathways related to HIF-1 and found both PI3K/AKT and MAPK/ERK were involved in the SYP-5 mediated invasive inhibition of Bcap37 cells. These results indicates that SYP-5 inhibits tumor cell migration and invasion, as well as tumor angiogenesis, which are mediated by suppressing PI3K/AKT- and MAPK/ERK-dependent HIF-1 pathway. It suggests that SYP-5 might be a potential HIF-1 inhibitor as an anticancer agent.

Identification of novel synaptonemal complex components in C. elegans

J Cell Biol 2020 May 4;219(5):e201910043.PMID:32211899DOI:10.1083/jcb.201910043.

The synaptonemal complex (SC) is a tripartite protein scaffold that forms between homologous chromosomes during meiosis. Although the SC is essential for stable homologue pairing and crossover recombination in diverse eukaryotes, it is unknown how individual components assemble into the highly conserved SC structure. Here we report the biochemical identification of two new SC components, SYP-5 and SYP-6, in Caenorhabditis elegans. SYP-5 and SYP-6 are paralogous to each other and play redundant roles in synapsis, providing an explanation for why these genes have evaded previous genetic screens. Superresolution microscopy reveals that they localize between the chromosome axes and span the width of the SC in a head-to-head manner, similar to the orientation of other known transverse filament proteins. Using genetic redundancy and structure-function analyses to truncate C-terminal tails of SYP-5/6, we provide evidence supporting the role of SC in both limiting and promoting crossover formation.

Multivalent weak interactions between assembly units drive synaptonemal complex formation

J Cell Biol 2020 May 4;219(5):e201910086.PMID:32211900DOI:10.1083/jcb.201910086.

The synaptonemal complex (SC) is an ordered but highly dynamic structure assembled between homologous chromosomes to control interhomologous crossover formation, ensuring accurate meiotic chromosome segregation. However, the mechanisms regulating SC assembly and dynamics remain unclear. Here, we identified two new SC components, SYP-5 and SYP-6, in Caenorhabditis elegans that have distinct expression patterns and form distinct SC assembly units with other SYPs through stable interactions. SYP-5 and SYP-6 exhibit diverse in vivo SC regulatory functions and distinct phase separation properties in cells. Charge-interacting elements (CIEs) are enriched in SC intrinsically disordered regions (IDRs), and IDR deletion or CIE removal confirmed a requirement for these elements in SC regulation. Our data support the theory that multivalent weak interactions between the SC units drive SC formation and that CIEs confer multivalency to the assembly units.

An Oxygen-Concentration-Controllable Multiorgan Microfluidic Platform for Studying Hypoxia-Induced Lung Cancer-Liver Metastasis and Screening Drugs

ACS Sens 2021 Mar 26;6(3):823-832.PMID:33657793DOI:10.1021/acssensors.0c01846.

Various cancer metastasis models based on organ-on-a-chip platforms have been established to study molecular mechanisms and screen drugs. However, current platforms can neither reveal hypoxia-induced cancer metastasis mechanisms nor allow drug screening under a hypoxia environment on a multiorgan level. We have developed a three-dimensional-culture multiorgan microfluidic (3D-CMOM) platform in which the dissolved oxygen concentration can be precisely controlled. An organ-level lung cancer and liver linkage model was established under normoxic/hypoxic conditions. A transcriptomics analysis of the hypoxia-induced lung cancer cells (A549 cells) on the platform indicated that the hypoxia-inducible factor 1α (HIF-1α) pathway could elevate epithelial-mesenchymal transition (EMT) transcription factors (Snail 1 and Snail 2), which could promote cancer metastasis. Then, protein detection demonstrated that HIF-1α and EMT transcription factor expression levels were positively correlated with the secretion of cancer metastasis damage factors alpha-fetoprotein (AFP), alkaline phosphatase (ALP), and gamma-glutamyl transpeptidase (γ-GT) from liver cells. Furthermore, the cancer treatment effects of HIF-1α inhibitors (tirapazamine, SYP-5, and IDF-11774) were evaluated using the platform. The treatment effect of SYP-5 was enhanced under the hypoxic conditions with fewer side effects, similar to the findings of TPZ. We can envision its wide application in future investigations of cancer metastasis and screening of drugs under hypoxic conditions with the potential to replace animal experiments.