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AdipoGen Life Sciences
SP600125
25
CHF
CHF 25.00
In stock
AG-CR1-3549-M0011 mgCHF 25.00
AG-CR1-3549-M0055 mgCHF 70.00
| Product Details | |
|---|---|
| Synonyms | Anthra[1-9-cd]pyrazol-6(2H)-one; 1,9-Pyrazoloanthrone; Pyrazolanthrone; NSC 75890 |
| Product Type | Chemical |
| Properties | |
| Formula |
C14H8N2O |
| MW | 220.2 |
| CAS | 129-56-6 |
| Purity Chemicals | ≥98% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (10mg/ml) or DMF (10mg/ml). Slightly soluble in ethanol (<1mg/ml). |
| InChi Key | ACPOUJIDANTYHO-UHFFFAOYSA-N |
| Smiles | O=C1C2=C3C(N([H])N=C3C4=C1C=CC=C4)=CC=C2 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light when in solution. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
- SP600125 is an orally active, reversible and ATP-competitive broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 (IC50 = 40nM, 40nM and 90nM, respectively). In Jurkat T cells, SP600125 suppressed the phosphorylation of c-Jun with IC50 of 5-10 μM. It has 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR.
- SP600125 is also a broad-spectrum inhibitor of serine/threonine kinases including hydrocarbon receptor (AhR), Mps1, Aurora kinase A, FLT3 and TRKA.
- SP600125 inhibits cell cycle, autophagy and ferroptosis and activates apoptosis. It shows anti-inflammatory activity by inhibiting the expression of inflammatory genes such as COX-2, IL-2 IFN-γ and TNF-α and has antiviral and neuroprotective properties.
- SP600125 demonstrated inhibitory effects on tumor cell proliferation, endothelial cell migration and tumor growth as well as blocking tumor and endothelial cells in the G2 phase of the cell cycle.
- SP600125 also promotes adipogenesis from MSCs and is an essential component of media for maintaining stem cells in naive pluripotent state.
- JNK1-mediated NLRP3 phosphorylation at S194 is a critical priming event and is essential for NLRP3 inflammasome activation. The JNK1 inhibitor SP600125 exhibits a robust inhibition of inflammasome activation.
Product References
- SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase: B.L. Bennett, et al.; PNAS 98, 13681 (2001)
- SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway: D. Vaishnav, et al.; BBRC 307, 855 (2003)
- The Jun N-terminal kinase inhibitor SP600125 is a ligand and antagonist of the aryl hydrocarbon receptor: A. Joiakim, et al.; Drug Metab. Dispos. 31, 1279 (2003)
- Targeting the JNK MAPK cascade for inhibition: basic science and therapeutic potential: M.A. Bogoyewitch, et al.; Biochim. Biophys. Acta Proteins & Proteomics 1697, 89 (2004) (Review)
- The neuroprotective action of SP600125, a new inhibitor of JNK, on transient brain ischemia/reperfusion-induced neuronal death in rat hippocampal CA1 via nuclear and non-nuclear pathways: Q.-H. Guan, et al.; Brain Res. 1035, 51 (2005)
- Inhibition of tumor growth, angiogenesis, and tumor cell proliferation by a small molecule inhibitor of c-Jun N-terminal kinase: B.W. Ennis, et al.; J. Pharmacol. Exp. Ther. 313, 325 (2005)
- Ablation of the spindle assembly checkpoint by a compound targeting Mps1: M. Schmidt, et al.; EMBO Rep. 6, 866 (2005)
- Induction of apoptosis and cell cycle arrest by a specific c-Jun NH2-terminal kinase (JNK) inhibitor, SP-600125, in gastrointestinal cancers: H.H. Xia, et al.; Cancer Lett. 241, 268 (2006)
- SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition: J.A. Kim, et al.; Oncogene 29, 1702 (2010)
- Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase: R. Colombo, et al.; Cancer Res. 70, 10255 (2010)
- SP600125, a JNK inhibitor, suppresses growth of JNK-inactive glioblastoma cells through cell-cycle G2/M phase arrest: J.Y. Li, et al.; Pharmazie 67, 942 (2012)
- Selective killing of p53-deficient cancer cells by SP600125: M. Jemaa, et al.; EMBO Mol. Med. 4, 500 (2012)
- Posttranslational modification of vesicular stomatitis virus glycoprotein, but not JNK inhibition, is the antiviral mechanism of SP600125: S. Marozin, et al.; J. Virol. 86, 4844 (2012)
- NLRP3 phosphorylation is an essential priming event for inflammasome activation: N. Song, et al.; Mol. Cell 68, 185 (2017)
- A six-inhibitor culture medium for improving naïve-type pluripotency of porcine pluripotent stem cells: Y. Yuan, et al.; Cell Death Disc. 5, 104 (2019)
- Zinc Oxide Nanoparticles Induce Ferroptotic Neuronal Cell Death in vitro and in vivo: X. Qin, et al.; Int. J. Nanomed. 15, 5299 (2020)
- Protective effects of SP600125 on mice infected with H1N1 influenza A virus: Y. Tang, et al.; Arch. Virol. 166, 2151 (2021)
- Inhibitors of c-Jun N-Terminal Kinase 3: P. Koch; Top Med. Chem. 36, 203 (2021) (Review)