- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable 3′-pyridyl oxindole compound that acts as a potent and reversible inhibitor of JAK3 (IC50 = 27 nM)and displays ~16-fold greater selectivity over JAK2. Binds to the enzyme active site and prevents IL-2-induced cellular phosphorylation of JAK3 and STAT5. Inhibits IL-2-induced cell proliferation (IC50 = 760 and 250 nM for mouse CTLL and human T-cells, respectively) and alleviates oxazolone-induced ear odema in mouse with an efficacy comparable to that of Dexamethasone (Cat. No. 265005).
A cell-permeable, potent, and reversible inhibitor of Janus kinase 3 (JAK3) (IC50 = 27 nM). Reported to bind to the enzyme active site and prevent IL-2-induced phosphorylation of JAK3 and STAT5. Also reported to inhibit IL-2-induced cell proliferation (IC50 = 760 nM for murine CTLL cells and 250 nM for human T-cells). Shown to alleviate oxazolone-induced ear edema in mice with an efficacy comparable to Dexamethasone (Cat. No. 265005) and displays ~16-fold greater selectivity over JAK2.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JAK-3
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chen, J., et al. 2006. Bioorg. Med. Chem. Lett. In press.
Adams, C., et al. 2003. Bioorg. Med. Chem. Lett.13, 3105.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| potency | 27 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| color | yellow |
| solubility | water: 1 mg/mL,DMSO: 5 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [S](=O)(=O)(O)C.[nH]1c(ccc1)\C=C2\c3c(ccc(c3)c4cnccc4)NC\2=O |
| InChI | 1S/C18H13N3O.CH4O3S/c22-18-16(10-14-4-2-8-20-14)15-9-12(5-6-17(15)21-18)13-3-1-7-19-11-13;1-5(2,3)4/h1-11,20H,(H,21,22);1H3,(H,2,3,4)/b16-10-; |
| InChI key | ZUDPNBZMAJGYTE-HYMQDMCPSA-N |
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