480401-M

NFAT Inhibitor, Cell-Permeable

The NFAT Inhibitor, Cell-Permeable controls the biological activity of NFAT. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): NFAT Inhibitor, Cell-Permeable, 11R-VIVIT, Nuclear Factor of Activated T cells Inhibitor, RRRRRRRRRRR-GGG- MAGPHPVIVITGPHEE, 11R-VIVIT, Nuclear Factor of Activated T cells Inhibitor, RRRRRRRRRRR-GGG-MAGPHPVIVITGPHEE
• Empirical Formula (Hill Notation): C₁₄₇H₂₅₉N₆₇O₃₆S
• Molecular Weight: 3573.12
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 1 mg/mL; DMSO: 5 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable version of NFAT Inhibitor (Cat. No. 480402) that is modified at the N-terminal with an eleven arginine transduction domain and a three glycine linker sequence. Prevents the activation and proliferation of T cells both in vitro ( ~ 43% at 1 µM using mixed lymphocyte cultures) and in vivo (10 mg/kg using C3H/HeN mice). Shown to be effective in providing immunosuppression in a murine islet xenograft model. Unlike Cyclosporin A (Cat. No. 239835) and FK506, 11R-VIVIT does not cause side effects outside the immune system as a result of calcineurin (Cat. No. 539568) inhibition and therefore serves as a less toxic alternative for in vivo applications. The functional half-life of 11R-VIVIT has been estimated to be ~30 h in Jurkat cells.

A cell-permeable version of NFAT Inhibitor (Cat. No. 480402) that is modified at the C-terminus with an 11-arginine transduction domain and a 3-glycine linker sequence. Prevents the activation and proliferation of T cells both in vitro (~43% at 1 µM using mixed lymphocyte cultures) and in vivo (10 mg/kg using C3H/HeN mice). Show to be effective in providing immunosuppression in a murine islet xenograft model. Unlike Cyclosporin A (Cat. No. 239835) and FK-506, 11R-VIVIT does not cause side effects outside the immune system as a result of calcineurin (Cat. No. 539568) inhibition, therefore serves as a less toxic alternative for animal studies. The functional half-life of 11R-VIVIT has been estimated to be ~30 h in Jurkat cells.

Application

Use at 1 µM for preventing the activation and proliferation of T cells

Biochem/physiol Actions

Primary Target
NFAT

Warning

Toxicity: Harmful (C)

Sequence

H-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Gly-Gly-Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu-OH

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Noguchi, H., et al. 2004. Nat. Med.10, 305.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable