Table 2.

Physicochemical characteristics of CaN/NFAT inhibitors.

Inhibitor	Characteristic profile
	Composition	Mode of action	Binding partner	IC50/Kd *	Side effects
CsA	A cyclic peptide of 11 amino acids	Complex blocks substrate access to the active centre of CaN	Cyclophilin	7 nM	Nephrotoxicity, hypertension, neurotoxicity
FK506	23-membered polyketide macrolide	Complex blocks substrate access to the active centre of CaN	FK506 binding protein (FKBP-12)	0.4 nM	Nephrotoxicity
VIVIT peptide	A 16 member linear L-peptide	Blocks CaN-NFATc interaction	No	0.5 µM* < 1 µM	Not observed
LxVP peptide	15 - mer peptide from NFATc1	Blocks CaN-NFATc interaction and regulates enzymatic activity of CaN	No	~ 0.3 µM	Not observed
Dipyridamole	Pyramidopyri-midine compound	Disrupts CaN-NFATc binding	No	~ 10 µM	Cytotoxicity, excitotoxicity under injurious conditions
INCA-6	Small organic molecule	Disrupts CaN-NFATc complex formation by covalent binding to CaN	No	~ 0.8 µM*	Cytotoxicity
A-28522	Small organic molecule	Inhibits NFAT activity	No	N/A	N/A
Q-134R	Hydroxyquinoline derivative	Partially inhbits NFAT activity	No	~ 400 nM	Not observed

N/A, not available.

*Kd.