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31 May 2012
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Leflunomide metabolite that blocks TNF-dependent NF-κB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-γ-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1β-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells. A cell-permeable, reversible, and substrate competitive inhibitor that inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3.
| Product information | |||
|---|---|---|---|
| Form | White solid | ||
| Primary Target | DHO-DH | ||
| Primary Target IC50 | 220 nM | ||
| Secondary target | IL-1b-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells | ||
| Molar mass | 270.2 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C12H9F3N2O2 | ||
| CAS number | 108605-62-5 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Carcinogenic / Teratogenic |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 22-36 Do not breathe dust. Wear suitable protective clothing. |
||
| R Phrase |
R: 40 Limited evidence of a carcinogenic effect. |
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