480403

NFAT Activation Inhibitor III

The NFAT Activation Inhibitor III, also referenced under CAS 3519-82-2, controls the biological activity of NFAT. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): NFAT Activation Inhibitor III, Inhibitor of NFAT- Calcineurin Association-6, INCA-6, Inhibitor of NFAT-Calcineurin Association-6, INCA-6
• Empirical Formula (Hill Notation): C₂₀H₁₂O₂
• CAS Number: 3519-82-2
• Molecular Weight: 284.31
• MDL number: MFCD00226933
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL (Use only fresh DMSO.), ethanol: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C1C2=C(C3c4c(cccc4)C2c5c3cccc5)C(=O)C=C1
• InChI: 1S/C20H12O2/c21-15-9-10-16(22)20-18-12-6-2-1-5-11(12)17(19(15)20)13-7-3-4-8-14(13)18/h1-10,17-18H
• InChI key: GCHPUOHXXCNSQL-UHFFFAOYSA-N

Description

General description

A cell-permeable quinone compound that acts as a potent and selective inhibitor of Calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling. Binds to calcineurin with high affinity (K_d = 800 nM), disrupts its interaction with NFAT and completely blocks its dephosphorylation, nuclear import of NFAT (~40 µM in C1.7W2 T cells), and induction of cytokine mRNAs. Unlike CsA (Cat. No. 239835) and FK506, INCA-6 does not affect calcineurin activity or its downstream signaling.

A cell-permeable, potent, and selective inhibitor of Calcineurin-NFAT (Nuclear Factor of Activated T cells) signaling. Binds to calcineurin with high affinity (K_d = 800 nM), disrupts its interaction with NFAT, and completely blocks calcineurin-dependent NFAT dephosphorylation, nuclear import (~40 µM in C1.7W2 T cells), and induction of NFAT-targeted cytokine mRNAs. Unlike CsA (Cat. No. 239835) and FK506, INCA-6 does not affect calcineurin activity or its downstream signaling.

Biochem/physiol Actions

Cell permeable: yes

Kd = 800 nM for calcineurin-NFAT

Primary Target
Calcineurin-NFAT

Product does not compete with ATP.

Reversible: no

Preparation Note

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

Other Notes

Roehrl, M.H.A., et al. 2004. Biochemistry43, 16067.
Roehrl, M.H.A., et al. 2004. Proc. Natl. Acad. Sci. USA101, 7554.

Legal Information

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable