SP600125

SKU
S-2022
  • CAS:129-56-6
  • Formula:C14H8N2O
  • MW:220.23 Da
  • Appearance:Yellow to green solid
  • Purity:>98.82%

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1

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Product Name Qty
SP600125
5 mg
$66.29
SP600125
50 mg
$178.49

Description

SP600125 is an anthrapyrazolone inhibitor that acts strongly on Jun N-terminal kinase (JNK). SP600125 exerts an inhibitory effect on JNK-1, -2 and -3, though higher concentrations are required for effective inhibition of JNK-3. Through JNK inhibition, SP600125 can prevent inflammatory genes from being expressed, as well as prevent differentiation of CD4 cells.

SP-600125 exhibits over 300-fold greater selectivity for JNK as compared to ERK1 and p38.

Applications

Studies of SP600125 have demonstrated its ability to significantly suppress epithelial cell apoptosis in mouse models. This suppression of apoptosis through JNK inhibition has also made SP600125 the target of research seeking novel neuroprotective agents to prevent ischemic brain injury. SP600125 has also played a role in various cell signaling studies, particularly those relating to MAP kinase signaling.

 

More Information
Alternate Name/Synonyms
Pyrazolanthrone, 1,9-Pyrazoloanthrone, Pyrazoleanthrone, JNK Inhibitor II, SAPK Inhibitor II, NSC 75890
SKU
S-2022
CAS #
129-56-6
Chemical Name
14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one
Chemical Formula
C14H8N2O
Molecular Weight
220.23 Da
Appearance
Yellow to green solid
Purity
>98.82%
Solubility
Soluble in DMSO (22 mg/mL) or ethanol (2 mg/mL)
Storage Temp
-20°C(3 years), 4°C (2 years)
THERAPEUTIC AREA
Not Available
USE
SP600125 is a potent, selective and reversible inhibitor of JNK1, JNK2 and JNK3. It inhibits competitively with ATP and causes a dose-dependent inhibition of the phosphorylation of c-Jun, and thereby the expression of inflammatory genes COX-2, IFN-γ, IL-2, TNF-α. It also blocks the activation and differentiation of primary human CD4 cell cultures.
RTECS
CB4585000
Handling
Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.
Certificate of Analysis 1
Certificate of Analysis 2
Certificate of Analysis 3
GHS PICTOGRAMS
Handling Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.
Citations Induction of DNA damage-inducible gene GADD45beta contributes to sorafenib-induced apoptosis in hepatocellular carcinoma cells
ERK1/2 activation is required for resveratrol-induced apoptosis in MDA-MB-231 cells
Mechanisms of 4-hydroxy-2-nonenal induced pro- and anti-apoptotic signaling
4-Hydroxynonenal self-limits fas-mediated DISC-independent apoptosis by promoting export of Daxx from the nucleus to the cytosol and its binding to Fas
BSP and RANKL induce osteoclastogenesis and bone resorption synergistically
CXCR4/SDF1 mediate hypoxia induced chondrosarcoma cell invasion through ERK signaling and increased MMP1 expression
Role of galectin-3 in mast cell functions: galectin-3-deficient mast cells exhibit impaired mediator release and defective JNK expression
Oncogenic Met receptor induces cell-cycle progression in Xenopus oocytes independent of direct Grb2 and Shc binding or Mos synthesis, but requires phosphatidylinositol 3-kinase and Raf signaling
Suppression of FOXM1 sensitizes human cancer cells to cell death induced by DNA-damage
Glycogen synthase kinase 3 beta (GSK3β) phosphorylates the RNAase III enzyme Drosha at S300 and S302
MicroRNA expression profiling identifies activated B cell status in chronic lymphocytic leukemia cells
Targeting Forkhead Box M1 (FOXM1) in Human Cancer
MicroRNAs in normal and malignant lymphocytes
Molecular mechanisms of myofibroblast differentiation and the role of TGF beta 1, TNF alpha, and thrombin signal transduction
OX-LDL INDUCES LONG-TERM PRO-INFLAMMATORY CYTOKINE PRODUCTION AND FOAM CELL FORMATION VIA EPIGENETIC REPROGRAMMING OF MONOCYTES
Airway smooth muscle CXCR3 ligand production: regulation by JAK-STAT1 and intracellular Ca²⁺
Imaging mitogen-activated protein kinase function in xenograft models of prostate cancer
Recognition of Coxiella burnetii by toll-like receptors and nucleotide-binding oligomerization domain-like receptors
Activation of the complement system by Coxiella burnetii
Shiga toxin 2 and flagellin from shiga-toxigenic Escherichia coli superinduce interleukin-8 through synergistic effects on host stress-activated protein kinase activation
Ethanol extract of Inonotus obliquus inhibits lipopolysaccharide-induced inflammation in RAW 264.7 macrophage cells
Enhanced Release of Monocyte Chemoattractant Protein-1 (MCP-1) by High Glucose and Free Fatty Acid and its Underlying Mechanism in MIN6 β cells
Matrix proteins from smoke-exposed fibroblasts are pro-proliferative
Modulation of morphogenesis by noncanonical Wnt signaling requires ATF/CREB family-mediated transcriptional activation of TGFbeta2
Central role of IL-6 receptor signal-transducing chain gp130 in activation of L-selectin adhesion by fever-range thermal stress
The small GTP-binding protein RhoA regulates c-jun by a ROCK-JNK signaling axis
Inhibition of PDE4B suppresses inflammation by increasing expression of the deubiquitinase CYLD
Constitutive CD40 signaling in B cells selectively activates the noncanonical NF-kappaB pathway and promotes lymphomagenesis
MyD88-deficient Hydra reveal an ancient function of TLR signaling in sensing bacterial colonizers
Polychaete trunk neuroectoderm converges and extends by mediolateral cell intercalation
Plasminogen kringle 5 induces apoptosis of brain microvessel endothelial cells: sensitization by radiation and requirement for GRP78 and LRP1
Mitochondrial dysfunction and reactive oxygen species imbalance promote breast cancer cell motility through a CXCL14-mediated mechanism
Extracellular signal-related kinase positively regulates ataxia telangiectasia mutated, homologous recombination repair, and the DNA damage response
8-Chloro-cyclic AMP-induced growth inhibition and apoptosis is mediated by p38 mitogen-activated protein kinase activation in HL60 cells
Tracker Dyes to Probe Mitochondrial Autophagy (Mitophagy) in Rat Hepatocytes
CD40 and OX40 ligand are differentially regulated on asthmatic airway smooth muscle
Cigarette smoke disrupts the integrity of airway adherens junctions through the aberrant interaction of p120-catenin with the cytoplasmic tail of MUC1
EGFR and IL-1 signaling synergistically promote keratinocyte antimicrobial defenses in a differentiation-dependent manner
Candida albicans and Candida parapsilosis induce different T-cell responses in human peripheral blood mononuclear cells
A novel role for RIP1 kinase in mediating TNFα production
Diesel exhaust particles induce oxidative stress, proinflammatory signaling, and P-glycoprotein up-regulation at the blood-brain barrier
Selective gene activation by spatial segregation of insulin receptor B signaling
The in vitro effects of resistin on the innate immune signaling pathway in isolated human subcutaneous adipocytes
ERα mediates alcohol-induced deregulation of Pol III genes in breast cancer cells
Overexpression of 15-lipoxygenase-1 induces growth arrest through phosphorylation of p53 in human colorectal cancer cells
c-Jun Kinase Is a Critical Signaling Molecule in a Neonatal Model of Group B Streptococcal Sepsis
Parvin-beta inhibits breast cancer tumorigenicity and promotes CDK9-mediated peroxisome proliferator-activated receptor gamma 1 phosphorylation
Asthmatic airway smooth muscle CXCL10 production: mitogen-activated protein kinase JNK involvement
Th1 cytokine-induced syndecan-4 shedding by airway smooth muscle cells is dependent on mitogen-activated protein kinases
TGF-β enhances deposition of perlecan from COPD airway smooth muscle
JNK- and IkappaB-dependent pathways regulate MCP-1 but not adiponectin release from artificially hypertrophied 3T3-L1 adipocytes preloaded with palmitate in vitro
LMP1 regulates periodontal ligament progenitor cell proliferation and differentiation
Apoptosis and necroptosis are induced in rainbow trout cell lines exposed to cadmium
Interleukin-1beta induces increased transcriptional activation of the transforming growth factor-beta-activating integrin subunit beta8 through altering chromatin architecture
Oct1 is a switchable, bipotential stabilizer of repressed and inducible transcriptional states
Transcription of the transforming growth factor beta activating integrin beta8 subunit is regulated by SP3, AP-1, and the p38 pathway
MKP1 regulates the induction of MUC5AC mucin by Streptococcus pneumoniae pneumolysin by inhibiting the PAK4-JNK signaling pathway
Lysophosphatidic acid regulates trafficking of beta2-adrenergic receptors: the Galpha13/p115RhoGEF/JNK pathway stimulates receptor internalization
NF-kappaB and not the MAPK signaling pathway regulates GADD45beta expression during acute inflammation
Hepatitis C core protein impairs insulin downstream signalling and regulatory role of IGFBP-1 expression
Identification, expression and functional characterization of the GRAL gene
Ghrelin augments the expressions and secretions of proinflammatory adipokines, VEGF120 and MCP-1, in differentiated 3T3-L1 adipocytes
Vitamin K3 (menadione)-induced oncosis associated with keratin 8 phosphorylation and histone H3 arylation
Endogenous oxidative stress, but not ER stress, induces hypoxia-independent VEGF120 release through PI3K-dependent pathways in 3T3-L1 adipocytes
Reactivation of latent HIV-1 in central memory CD4⁺ T cells through TLR-1/2 stimulation
LPS induces IL-10 production by human alveolar macrophages via MAPKinases- and Sp1-dependent mechanisms
Involvement of c-Jun NH2-terminal kinase and nitric oxide-mediated mitochondria-dependent intrinsic pathway signaling in cardiotoxin-induced muscle cell death: role of testosterone
Staurosporine-induced cell death in salmonid cells: the role of apoptotic volume decrease, ion fluxes and MAP kinase signaling
Expression of the homeobox gene, HOPX, is modulated by cell differentiation in human keratinocytes and is involved in the expression of differentiation markers
Transforming growth factor beta1-mediated activation of the smooth muscle alpha-actin gene in human pulmonary myofibroblasts is inhibited by tumor necrosis factor-alpha via mitogen-activated protein kinase kinase 1-dependent induction of the Egr-1 transcriptional repressor
REIC/Dkk-3 overexpression downregulates P-glycoprotein in multidrug-resistant MCF7/ADR cells and induces apoptosis in breast cancer
Nonclassical pathway of Pseudomonas aeruginosa DNA-induced interleukin-8 secretion in cystic fibrosis airway epithelial cells
Apoptosis induction in human lung adenocarcinoma cells by oil-soluble allyl sulfides: triggers, pathways, and modulators
CagA phosphorylation-dependent MMP-9 expression in gastric epithelial cells
Heme oxygenase-1 signals are involved in preferential inhibition of pro-inflammatory cytokine release by surfactin in cells activated with Porphyromonas gingivalis lipopolysaccharide
Hypoxia activates c-Jun N-terminal kinase via Rac1-dependent reactive oxygen species production in hepatocytes
Inhibition of the proliferation and invasion of hepatocellular carcinoma cells by lipocalin 2 through blockade of JNK and PI3K/Akt signaling
Ethyl linoleate from garlic attenuates lipopolysaccharide-induced pro-inflammatory cytokine production by inducing heme oxygenase-1 in RAW264.7 cells
Schisandra chinensis α-iso-cubebenol induces heme oxygenase-1 expression through PI3K/Akt and Nrf2 signaling and has anti-inflammatory activity in Porphyromonas gingivalis lipopolysaccharide-stimulated macrophages
Regulatory role of the JNK-STAT1/3 signaling in neuronal differentiation of cultured mouse embryonic stem cells
Upregulation of heme oxygenase-1 via PI3K/Akt and Nrf-2 signaling pathways mediates the anti-inflammatory activity of Schisandrin in Porphyromonas gingivalis LPS-stimulated macrophages
Differential regulation of Streptococcus pneumoniae-induced human MUC5AC mucin expression through distinct MAPK pathways
In vivo and in vitro characterization of the immune stimulating activity of the Neisserial porin PorB
Advanced glycation end products induce human corneal epithelial cells apoptosis through generation of reactive oxygen species and activation of JNK and p38 MAPK pathways
Proteasome activity influences UV-mediated subnuclear localization changes of NPM
Involvement of skeletal muscle gene regulatory network in susceptibility to wound infection following trauma
Visfatin is regulated by rosiglitazone in type 2 diabetes mellitus and influenced by NFκB and JNK in human abdominal subcutaneous adipocytes
Cytoprotective effects of phlorofucofuroeckol A isolated from Ecklonia stolonifera against tacrine-treated HepG2 cells
Possible involvement of PI3K-dependent pathways in the increased VEGF120 release from osteoblastic cells preloaded with palmitate in vitro
Inhibition of mitogen activated protein kinases increases the sensitivity of A549 lung cancer cells to the cytotoxicity induced by a kava chalcone analog
Apoptosis of mink lung epithelial cells by co-treatment of low-dose staurosporine and transforming growth factor-beta1 depends on the enhanced TGF-beta signaling and requires the decreased phosphorylation of PKB/Akt
Exploring a common mechanism of alcohol-induced deregulation of RNA Pol III genes in liver and breast cells
Elk1 and AP-1 sites in the TBP promoter mediate alcohol-induced deregulation of Pol III-dependent genes
Curcumin exerts antitumor effects in retinoblastoma cells by regulating the JNK and p38 MAPK pathways
Dexamethasone inhibits the Nox-dependent ROS production via suppression of MKP-1-dependent MAPK pathways in activated microglia
Estrogen-independent effects of ER-α36 in ER-negative breast cancer
JNK/SAPK and p38 SAPK-2 mediate mechanical stretch-induced apoptosis via caspase-3 and -9 in NRK-52E renal epithelial cells
Bluetongue virus infection: activation of the MAP kinase-dependent pathway is required for apoptosis
A case of excessive autophagocytosis with multiorgan involvement and low clinical penetrance
Copper-induced stimulation of extracellular signal-regulated kinase in trout hepatocytes: the role of reactive oxygen species, Ca2+, and cell energetics and the impact of extracellular signal-regulated kinase signaling on apoptosis and necrosis
Cytoplasmic accumulation of the RNA binding protein HuR is central to tamoxifen resistance in estrogen receptor positive breast cancer cells
The HLA-B associated transcript 1 (BAT1) expression in human adipose tissue: BAT1 modulation with increasing adiposity and diabetes
Genome-Wide Angiotensin Ii Regulated Microrna Expression Profiling; A Smooth Muscle-Specific Microrna Signature
Selective insulin signaling in the pancreatic beta-cell via the two insulin receptor isoforms
Targeting angiogenesis with plasminogen kringle 5
The Function and Regulation of LIM Domain Mineralization Protein (LMP) in Periodontal Ligament Progenitor Cells.
Towards understanding the benefits, establishment and maintenance of host-microbe homeostasis in Hydra
Comparative molecular and morphogenetic characterisation of larval body regions in the polychaete annelid Platynereis dumerilii
Load Down-Regulates TNF-Alpha Induced Cartilage Degradation in Part Through NF-KB and P38 Pathways
Untersuchungen zur Pathogenität von Helicobacter hepaticus: genomische und funktionelle Aspekte
Fibronectin modulates acinar morphogenesis by controlling mammary epithelial cell growth
タモギタケ熱水抽出物の抗カンジダ菌効果および上皮細胞における β ディフェンシン発現増強作用
Mechanisms of B cell activation and lymphomagenesis
Functional proteomics of Arabidopsis thaliana guard cells uncovers new stomatal signaling pathways
PKC-delta controls the fMLF-induced overproduction of superoxide by neutrophils
Ultrafine carbon particles induce apoptosis and proliferation in rat lung epithelial cells via specific signaling pathways both using EGF-R
Mechanisms of serum potentiation of GM-CSF production by human airway smooth muscle cells
Mechanisms of low-density lipoprotein-induced expression of connective tissue growth factor in human aortic endothelial cells
Redox control of manumycin A-induced apoptosis in anaplastic thyroid cancer cells: Involvement of the xenobiotic apoptotic pathway
FcαRI-mediated inhibition of IL-12 production and priming by IFN-γ of human monocytes and dendritic cells
Neuroprotection with pioglitazone against LPS insult on dopaminergic neurons may be associated with its inhibition of NF-kappaB and JNK activation and suppression of COX-2 activity
THE EFFECT OF PPARγ ACTIVATION BY PIOGLITAZONE ON THE LIPOPOLYSACCHARIDE-INDUCED PGE2 AND NO PRODUCTION: POTENTIALUNDERLYING ALTERATION OF SIGNALING TRANSDUCTION
IKAP/Elp1 involvement in cytoskeleton regulation and implication for familial dysautonomia
The Pseudomonas aeruginosa HSP70-like protein DnaK induces IL-1β expression via TLR4-dependent activation of the NF-κB and JNK signaling pathways
Benzydamine inhibits osteoclast differentiation and bone resorption via down-regulation of interleukin-1β expression
The significance of Runx2 mediating alcohol-induced Brf1 expression and RNA Pol III gene transcription
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