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JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2, the ZAP/SYK family tyrosine kinase SYK, the TEC family tyrosine kinase BTK, the SRC family tyrosine kinase LYN, or the receptor family tyrosine kinase insulin receptor kinase, even at concentrations as high as 350 μM. JANEX-1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19 but not in melanoma (M24-MET) or squamous carcinoma (SQ20B) cells.
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Source | PLoS One (2016). Figure 1. JANEX-1 |
| Method | flow cytometry | |
| Cell Lines | human blood T lymphocytes | |
| Concentrations | 80 μM | |
| Incubation Time | 5, 24 or 48 h | |
| Results | Both PP2 and WHI-P131decreased the number of CD25+ cells in PHA-induced cultures, reduced the S-phase induction and suppressed the growth of activated PBL |
| Molecular Weight | 297.31 |
| Formula | C16H15N3O3 |
| CAS Number | 202475-60-3 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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