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Submit ReviewSP 600125
说明： Selective JNK inhibitor
化学名： Anthra[1-9-cd]pyrazol-6(2H)-one
纯度： ≥98% (HPLC)
生物活性 for SP 600125
SP 600125 is a selective JNK inhibitor. Competitively and reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38β and a range of enzymes. Active in vivo. Exhibits reduced selectivity over other protein kinases under certain conditions. SP 600125 protects renal tubular epithelial cells from ischemia/reperfusion-induced apoptosis. Promotes chondrogenesis of bone mesenchymal stem cells by inhibition of TNF-α-induced inflammation. Adipogenesis from MSCs is also promoted by SP 600125. Essential component of medium for maintaining stem cells in naive pluripotent state.
技术数据 for SP 600125
| 分子量 | 220.23 |
| 公式 | C14H8N2O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 129-56-6 |
| PubChem ID | 8515 |
| InChI Key | ACPOUJIDANTYHO-UHFFFAOYSA-N |
| Smiles | O=C1C2=C3C(NN=C3C3=CC=CC=C13)=CC=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SP 600125
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 22.02 | 100 |
制备储备液 for SP 600125
以下数据基于产品分子量 220.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.54 mL | 22.7 mL | 45.41 mL |
| 5 mM | 0.91 mL | 4.54 mL | 9.08 mL |
| 10 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 50 mM | 0.09 mL | 0.45 mL | 0.91 mL |
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产品说明书 for SP 600125
参考文献 for SP 600125
参考文献是支持产品生物活性的出版物。
Bennett et al (2001) SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc.Natl.Acad.Sci.U.S.A. 98 13681 PMID: 11717429
Schnabl et al (2001) TAK1/JNK and p38 have opposite effects on rat hepatic stellate cells. Hepatology 34 953 PMID: 11679966
Wang et al (2007) SP600125, a selective JNK inhibitor, protects ischemic renal injury via suppressing the extrinsic pathways of apoptosis. Life Sci. 80 2067 PMID: 17459422
Zhao et al (2013) Activation of JNKs is essential for BMP9-induced osteogenic differentiation of mesenchymal stem cells. BMB Rep. 46 422 PMID: 23977991
Ding et al (2021) SP600125 restored TNF-α-induced impaired chondrogenesis in bone mesenchymal stem cells and its antiosteoarthritis effect in mice. Stem Cells Dev. 30 1028 PMID: 34486378
Tominaga et al (2005) Negative regulation of adipogenesis from human mesenchymal stem cells by Jun N-terminal kinase. Biochem.Biophys.Res.Commun. 326 499 PMID: 15582605
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关键词: SP 600125, SP 600125 supplier, selective, JNK, inhibitors, inhibits, MAPK, Signaling, Signalling, c-Jun, N-Terminal, Kinase, SAPKs, Stress-Activated, Protein, Mitogen-Activated, SP600125, JNK/c-jun, Mesenchymal, Stem, Cells, Cell, Proliferation, 1496, Tocris Bioscience
108 篇 SP 600125 的引用文献
引用文献是使用了 Tocris 产品的出版物。 SP 600125 的部分引用包括：
Wan et al (2018) Suppressive effects of berberine on atherosclerosis via downregulating visfatin expression and attenuating visfatin-induced endothelial dysfunction. Int J Mol Med 41 1939 PMID: 29393413
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Hsu et al (2011) JNK suppression is essential for 17β-OE inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells. PLoS One 18 61 PMID: 21859479
Kim et al (2011) Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells. Nat Commun 15 211 PMID: 21994479
Balboa et al (2018) Ins. mutations impair beta-cell development in a patient-derived iPSC model of neonatal diabetes. Elife 7 PMID: 30412052
Kang et al (2018) Improving Cell Survival in Injected Embryos Allows Primed Pluripotent Stem Cells to Generate Chimeric Cynomolgus Monkeys. Cell Rep 25 2563 PMID: 30485820
Maronde (2018) Trehalose Activates CRE-Dependent Transcriptional Signaling in HT22 Mouse Hippocampal Neuronal Cells: A Central Role for PKA Without cAMP Elevation. Front Mol Neurosci 11 386 PMID: 30405349
Lin et al (2018) Capsaicin-induced TRIB3 upregulation promotes apoptosis in cancer cells. Cancer Manag Res 10 4237 PMID: 30323679
Yang et al (2017) Derivation of Pluripotent Stem Cells with In Vivo Embryonic and Extraembryonic Potency. Cell 169 243 PMID: 28388409
Harada et al (2017) Focal Adhesion Kinase Promotes the Progression of Aortic Aneurysm by Modulating Macrophage Behavior. Arterioscler Thromb Vasc Biol 37 156 PMID: 27856458
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Gonsalves et al (2014) Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α. Am J Hematol 89 273 PMID: 24227191
Bae et al (2014) Activation of pattern recognition receptors in brown adipocytes induces inflammation and suppresses uncoupling protein 1 expression and mitochondrial respiration. Am J Physiol Cell Physiol 306 C918 PMID: 24627558
Basu et al (2014) Suppression of MAPK/JNK-MTORC1 signaling leads to premature loss of organelles and nuclei by autophagy during terminal differentiation of lens fiber cells. Autophagy 10 1193 PMID: 24813396
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Enomoto et al (2013) Transcriptional regulation of an Ins-sensitizing adipokine adipolin/CTRP12 in adipocytes by Krüppel-like factor 15. Am J Physiol Lung Cell Mol Physiol 8 e83183 PMID: 24358263
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García-Escudero et al (2008) Glioma regression in vitro and in vivo by a suicide combined treatment. Exp Cell Res 6 407 PMID: 18337448
Zhou (2017) TNFα induces tolerant production of CXC chemokines in colorectal cancer HCT116 cells via A20 inhibition of ERK signaling. Int Immunopharmacol 54 296 PMID: 29175508
Martin et al (2014) miR-155 induced transcriptome changes in the MCF-7 breast cancer cell line leads to enhanced mitogen activated protein kinase signaling. Korean J Physiol Pharmacol 5 353 PMID: 25352952
Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. Steroids 5 4421 PMID: 25030704
El-Sayed et al (2014) P2Y2 nucleotide receptor activation enhances the aggregation and self-organization of dispersed salivary epithelial cells. J Cell Mol Med 307 C83 PMID: 24760984
Xiong et al (2013) Arginase-II induces vascular smooth muscle cell senescence and apoptosis through p66Shc and p53 independently of its l-arginine ureahydrolase activity: implications for atherosclerotic plaque vulnerability. J Am Heart Assoc 2 e000096 PMID: 23832324
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Zhou and Too (2011) Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth. Arthritis Rheum 6 e21680 PMID: 21738764
Jezierska-Drutel et al (2019) The peroxidase PRDX1 inhibits the activated phenotype in mammary fibroblasts through regulating c-Jun N-terminal kinases. BMC Cancer 19 812 PMID: 31419957
Ulzii et al (2019) Scratching Counteracts IL-13 Signaling by Upregulating the Decoy Receptor IL-13Rα2 in Keratinocytes. Int J Mol Sci 20 PMID: 31284553
Zhen et al (2019) Purpurogallin Protects Keratinocytes from Damage and Apoptosis Induced by Ultraviolet B Radiation and Particulate Matter 2.5. Biomol Ther (Seoul) 27 395 PMID: 30419635
Wu (2017) TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells. Arch Biochem Biophys 622 26 PMID: 28442401
Han (2017) Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation. Brain Res 1663 132 PMID: 28322749
Yuri et al (2015) Maintenance of Mouse Nephron Progenitor Cells in Aggregates with Gamma-Secretase Inhibitor. PLoS One 10 e0129242 PMID: 26075891
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Yun et al (2009) AMP kinase signaling determines whether c-Jun N-terminal kinase promotes survival or apoptosis during glucose deprivation. Carcinogenesis 30 529 PMID: 19037093
Steubesand et al (2009) The expression of the beta-defensins hBD-2 and hBD-3 is differentially regulated by NF-kappaB and MAPK/AP-1 pathways in an in vitro model of Candida esophagitis. BMC Immunol 10 36 PMID: 19523197
Yeligar et al (2009) Ethanol augments RANTES/CCL5 expression in rat liver sinusoidal endothelial cells and human endothelial cells via activation of NF-kappa B, HIF-1 alpha, and AP-1. J Immunol 183 5964 PMID: 19828633
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Pervolaraki et al (2017) Type I and Type III IF.s Display Different Dependency on Mitogen-Activated Protein Kinases to Mount an Antiviral State in the Human Gut. Front Immunol 8 459 PMID: 28484457
Sidhar and Giri (2017) Induction of Bex genes by curcumin is associated with apoptosis and activation of p53 in N2a neuroblastoma cells. Sci Rep 7 41420 PMID: 28145533
Martínez-Sánchez et al (2017) Hypothalamic AMPK-ER Stress-JNK1 Axis Mediates the Central Actions of Thyroid Hormones on Energy Balance. Cell Metab 26 212 PMID: 28683288
Chang et al (2016) Derivation of Patient Specific Pluripotent Stem Cells Using Clinically Discarded Cumulus Cells. PLoS One 11 e0165715 PMID: 27802323
Abedini et al (2016) WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling. FASEB J 30 1534 PMID: 26667040
Nalvarte et al (2016) Estrogen receptor β controls MMP-19 expression in mouse ovaries during ovulation. Reproduction 151 253 PMID: 26700939
Suk et al (2013) A Taiwanese Propolis Derivative Induces Apoptosis through Inducing Endoplasmic Reticular Stress and Activating Transcription Factor-3 in Human Hepatoma Cells. Evid Based Complement Alternat Med 2013 658370 PMID: 24222778
Berdichevsky et al (2013) PI3K-Akt signaling activates mTOR-mediated epileptogenesis in organotypic hippocampal culture model of post-traumatic epilepsy. J Neurosci 33 9056 PMID: 23699517
Wong et al (2010) Bone morphogenic protein-4 impairs endothelial function through oxidative stress-dependent cyclooxygenase-2 upregulation: implications on hypertension. Circ Res 107 984 PMID: 20724703
Sutcliffe et al (2009) Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1. Br J Pharmacol 157 436 PMID: 19371341
Kim et al (2018) Enhanced Glycolysis Supports Cell Survival in EGFR-Mutant Lung Adenocarcinoma by Inhibiting Autophagy-Mediated EGFR Degradation. Cancer Res 78 4482 PMID: 29945964
Rahman et al (2016) 18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis. Biochemical Pharmacology 117 97 PMID: 27520483
Karmakar et al (2015) Neutrophil IL-1β processing induced by pneumolysin is mediated by the NLRP3/ASC inflammasome and caspase-1 activation and is dependent on K+ efflux. Nat Commun 194 1763 PMID: 25609842
Liu et al (2015) Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment. Int J Mol Sci 5 79 PMID: 25999956
Yoshimura et al (2015) Inhibitory effect of STAT on inflammation-related pathways in human abdominal aortic aneurysm tissue. Biomed Res Int 16 11213 PMID: 25993292
Chen et al (2015) Black Rice Anthocyanins Suppress Metastasis of Breast Cancer Cells by Targeting RAS/RAF/MAPK Pathway. Int J Clin Exp Pathol 2015 414250 PMID: 26649302
Bulut et al (2015) Effects of jnk inhibitor on inflammation and fibrosis in the ovary tissue of a rat model of polycystic ovary syndrome. Exp Hematol Oncol 8 8774 PMID: 26464620
Koerber et al (2015) Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma. Nat Commun 4 21 PMID: 26251761
Yang et al (2015) Inhibition of G9a Histone Methyltransferase Converts Bone Marrow Mesenchymal Stem Cells to Cardiac Competent Progenitors. PLoS One 2015 270428 PMID: 26089912
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Sommerfeld et al (2015) Free fatty acids shift Ins-induced hepatocyte proliferation towards CD95-dependent apoptosis. J Biomed Sci 290 4398 PMID: 25548285
Huang et al (2013) The role of bioactive nanofibers in enamel regeneration mediated through integrin signals acting upon C/EBPα and c-Jun. Biomaterials 34 3303 PMID: 23398885
Kook et al (2013) Fibroblast growth factor-4 enhances proliferation of mouse embryonic stem cells via activation of c-Jun signaling. PLoS One 8 e71641 PMID: 23967228
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Meotti et al (2012) Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways. Br J Pharmacol 166 1127 PMID: 22220695
Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832 PMID: 22434859
Lin et al (2012) Desipramine protects neuronal cell death and induces heme oxygenase-1 expression in Mes23.5 DArgic neurons. PLoS One 7 e50138 PMID: 23209658
Khuituan et al (2012) Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice. Am J Physiol Endocrinol Metab 302 E903 PMID: 22275752
Zhou et al (2010) miR-155 and its star-form partner miR-155* cooperatively regulate type I IF. production by human plasmacytoid dendritic cells. Blood 116 5885 PMID: 20852130
Ishida et al (2010) Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish. Dev Biol 340 468 PMID: 20144602
Lee et al (2010) Prevention of premature senescence requires JNK regulation of Bcl-2 and reactive oxygen species. Oncogene 29 561 PMID: 19855432
Zuco et al (2004) Induction of apoptosis and stress response in ovarian carcinoma cell lines treated with ST1926, an atypical retinoid. Cell Death Differ 11 280 PMID: 14657960
Holzberg et al (2003) Disruption of the c-JUN-JNK complex by a cell-permeable peptide containing the c-JUN delta domain induces apoptosis and affects a distinct set of interleukin-1-induced inflammatory genes. J Biol Chem 278 40213 PMID: 12832416
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Campàs et al (2003) Acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes. Cell Death Differ 101 3674 PMID: 12522004
Lee et al (2005) Estrogen receptor alpha pathway is involved in the regulation of Calbindin-D9k in the uterus of immature rats. Toxicol Sci 84 270 PMID: 15635152
Hoffmann et al (2005) MEK1-dependent delayed expression of Fos-related antigen-1 counteracts c-Fos and p65 NF-kappaB-mediated interleukin-8 transcription in response to cytokines or growth factors. J Biol Chem 280 9706 PMID: 15615716
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Yun et al (2005) Glucose deprivation increases mRNA stability of vascular endothelial growth factor through activation of AMP-activated protein kinase in DU145 prostate carcinoma. Blood 280 9963 PMID: 15640157
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Role of JNK activation in chemotherapy-induced apoptosis.
By
MARINA KOUTSIOUMPA on 05/31/2021
分析类型： In Vitro
种属： Human
Human cancer cells were pretreated for 2 hours with SP600125 before addition of chemotherapeutics and were incubated for 72 hours. SP600125 was used at 1, 3 and 10 μM. Real time apoptosis assays were performed. JNK inhibition partially reversed the chemotherapeutics-induced cellular apoptosis.
JNK inhibition in LPA induced pro-inflammatory phenotype in microglia..
By
lisha joshi on 06/10/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： Primary murine microglia cells
Primary murine microglia were treated with LPA (1µM) in the presence or absence of SP600125 (10µM) in order to investigate the role of JNK pathway in the LPA induced inflammatory phenotype. The inhibitor was well tolerated by the cells. DMSO was used as a vehicle control. Cells were lysed and collected for WB analysis in order to identify changes in the expression of COX2 and Arg1.
SP 600125 inhibits JNK activation in HOCl-LDL treated cardiomyocytes.
By
Chintan Koyani on 10/13/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： HL-1 cardiomyocytes
HL-1 cardiomyocytes were treated with SP 600125 (5 or 10 μM, 30 min) followed by 500 μg/ml HOCl-LDL (oxidant:lipoprotein molar ratio=800:1) for 1 h to follow pJNK expression using Western blot. SP 600125 at 10 μM concentration, completely inhibited activation of JNK.
JNK inhibition in BV2 microglia.
By
Joanna Plastira on 10/10/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： BV2 microglia
The inhibitor was used at a concentration of 10µM in BV2 microglia cell line. SP600125 inhibited the LPA induced activation of transcription factors (western blotting). It was also used in flow cytometry, ELISAs, IF and functional assays. The results were constant and reproducible.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for SP 600125
