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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C20H12O2
CAS Number:
Molecular Weight:
284.31
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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Quality Level

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

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 (Kd = 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 (Kd = 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)


Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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