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.

• Synonym(s): JAK3 Inhibitor VII, AD412, N-(Pyridin-4-yl)-3-[1-(4-chlorobenzyl)indol-3-yl]-propanamide
• Empirical Formula (Hill Notation): C₂₃H₂₀ClN₃O
• CAS Number: 796041-65-1
• Molecular Weight: 389.88
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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
• storage temp.: 2-8°C

Description

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

Warning

Toxicity: Standard Handling (A)

Other Notes

Carbonnelle, D., et al. 2009. J. Pharm. Exp. Ther.331, 710.
Carbonnelle, D., et al. 2007. Eur. J. Med. Chem.42, 686.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable