420145
JAK3 Inhibitor VII, AD412
The JAK3 Inhibitor VII, AD412, also referenced under CAS 796041-65-1, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
JAK3 Inhibitor VII, AD412, N-(Pyridin-4-yl)-3-[1-(4-chlorobenzyl)indol-3-yl]-propanamide
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable indole-3-propanamide immunosuppressant that is shown to selectively inhibit the kinase activity of JAK3 (by 81% and 36% at 90 and 30 µM, respectively) over that of JAK2 (by 29% and 0% at 90 and 30 µM, respectively) and reduce JAK1/3-dependent phosphorylations of Akt, STAT5a/b, and Erk1/2 in IL-2-stimulated CTL-L2 cells, but not JAK1/2-dependent STAT1 phosphorylation in INF-γ-stimulated U266 cultures. Reported to inhibit ConA-stimulated murine splenocytes and PHA-stimulated human PBL proliferation (IC50 = 17 and 25 µM, respectively) in vitro and be efficacious in ameliorating delayed hypersensitivity reaction in mice (by ~78% with a daily oral dose of 50 mg/kg) and in prolonging the survival of heart transplant-recipient rats (by >3-fold with 60 mg/kg/day, p.o.) in vivo.
Packaging
Packaged under inert gas
Other Notes
Carbonnelle, D., et al. 2009. J. Pharm. Exp. Ther.331, 710.
Carbonnelle, D., et al. 2007. Eur. J. Med. Chem.42, 686.
Carbonnelle, D., et al. 2007. Eur. J. Med. Chem.42, 686.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
相关内容
The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.
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