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| | 1,9-Pyrazoloanthrone Basic information |
| | 1,9-Pyrazoloanthrone Chemical Properties |
| Melting point | 281~282℃ | | Boiling point | 361.16°C (rough estimate) | | density | 1.1702 (rough estimate) | | refractive index | 1.5910 (estimate) | | storage temp. | 2-8°C | | solubility | H2O: insoluble | | pka | 11.75±0.20(Predicted) | | form | Yellowish orange solid | | color | yellow | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months | | InChIKey | ACPOUJIDANTYHO-UHFFFAOYSA-N | | CAS DataBase Reference | 129-56-6(CAS DataBase Reference) | | EPA Substance Registry System | Anthra[1,9-cd]pyrazol-6(2H)-one (129-56-6) |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 | | RTECS | CB4585000 | | TSCA | Yes | | HS Code | 29339900 | | Toxicity | LD50 ivn-mus: 178 mg/kg CSLNX* NX#00640 |
| | 1,9-Pyrazoloanthrone Usage And Synthesis |
| Description | SP-600125 (129-56-6) is a selective inhibitor of c-Jun N-terminal kinase (JNK). Reversibly inhibits JNK1,2 and 3 (IC50‘s range from 40-90 nM). >300-fold selectivity for JNK as compared to related MAP kinases. Anti-inflammatory activity. SP-600125 inhibits expression of presenilin-1 and Notch signaling in mouse brain. Cell permeable and active in vivo. | | Uses | C2C12 myoblasts were treated with SP600125 to test the stimulation of myogenesis.11 It was used to treat HepG2 cells to test the effects on oxysterol-induced necrosis.12 | | Uses | A broad-spectrum serine/threonine kinase inhibitor of JNK with an IC50 range from 40 to 90 nM. | | Uses | SP 600125 is a Jun N-terminal kinase (JNK) inhibitor. | | Definition | ChEBI: A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase. | | General Description | A potent, cell-permeable, selective, and reversible inhibitor of c-Jun N-terminal kinase (JNK) (IC50 = 40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3). The inhibition is competitive with respect to ATP. Exhibits over 300-fold greater selectivity for JNK as compared to ERK1 and p38-2 MAP kinases. Inhibits the phosphorylation of c-Jun and blocks the expression of IL-2, IFN-γ, TNF-α, and COX-2 in cells. Blocks IL-1-induced accumulation of phospho-Jun and induction of c-Jun transcription. | | Biological Activity | Selective inhibitor of c-Jun N-terminal kinase (JNK). Competitively and reversibly inhibits JNK1, 2 and 3 (IC 50 = 40-90 nM) with negligible activity at ERK2, p38 β and a range of enzymes (IC 50 > 10 μ M). Active in vivo . Shown to have reduced selectivity over other protein kinases under certain conditions. Protects renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis. Also available as part of the MAPK Inhibitor Tocriset™ . | | Biochem/physiol Actions | SP600125 is an anthrapyrazolone inhibitor of JNK that competes with ATP to inhibit the phosphorylation of c-Jun. It prevents the activation of inflammatory genes such as COX-2, IL-2 IFN-γ and TNF-α.8,9 It prevents the activation of JNK after brain ischemia and may be effective in treatment of ischemic stroke.10 | | Safety Profile | Poison by intravenous route.When heated to decomposition it emits toxic fumes ofNOx. | | storage | -20°C (desiccate) | | References | 1)Bennett et al. (2001), SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase; Proc. Natl. Acad. Sci. USA., 98 13681
2) Rahman et al. (2012), Intraperitoneal injection of JNK-specific inhibitor SP600125 inhibits the expression of presenilin-1 and Notch signaling in mouse brain without induction of apoptosis; Brain Res., 1448 117 |
| | 1,9-Pyrazoloanthrone Preparation Products And Raw materials |
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