Table 1 Low molecular weight inhibitors of calcineurin-NFATc signalling

General protein phosphatase inhibitors inhibiting also calcineurin (CaN)

Endothall

binds to the active centre of PP1, PP2A, CaN

11,5 μM** ^a

Tatlock JH 1997 [195]

FMPP

binds covalently to the active centre of PP1, PP2A, CaN

44 mM^b

Born TL 1995 [88]

Norcantharidin

binds to the active centre of PP1, PP2A, CaN

31 μM^b

Steward SG 2007 [90]

Okadaic acid

binds to the active centre of PP1, PP2A, CaN

4.6 μM^b

Bialojan C 1988 [196]

Tyrphostins

bind possibly to the active centre of PP1, PP2A, CaN

21 - 62 μM^b

Martin BL 1998 [89]

Inhibitors of calcineurin-dependent signalling - CsA, FK506 and derivatives

CsA/CypA

complex blocks substrate access to the active centre of CaN

7 nM^a

Fruman DA 1992 [197]

ISA247/CypA

complex blocks substrate access to the active centre of CaN

~100 nM^a

Aspeslet L 2001 [75]

[Dat-Sar]³-CsA

blocks substrate access to CaN independent of CypA

Baumgrass R 2004 [73]

FK506/FKBP12

complex blocks substrate access to the active centre of CaN

0.4 nM^a

Fruman DA 1992 [197]

Ascomycin/FKBP12

complex blocks substrate access to the active centre of CaN

0.7 nM^m

Sinclair PJ 1996 [198]

Pimecrolimus/FKBP12

complex blocks substrate access to the active centre of CaN

0.4 nM^a

Grassberger M 1999 [82]

Inhibitors of calcineurin-dependent signalling - alternative inhibitory compounds

1,5-dibenzoyloxymethyl-norcantharidin

binds to the active centre of CaN

7 μM^a

Baba Y 2003 [101]

AM404

inhibits NFATc-DNA binding

10 μM^c

Caballero FJ 2007 [132]

BTP1

inhibits of NFATc dephosphorylation in cells

60 nM^d

Trevillyan JM 2001 [118]

BTP2

decreases Ca²⁺ influx into cytosol

10 nM^c

Ishikawa J 2003 [119]

Dibefurin

inhibits enzymatic activity of CaN

44 μM^e

Brill GM 1996 [110]

Dipyridamole

disrupts CaN-NFATc binding

~10 μM^a

Mulero C 2009 [111]

Gossypol

inhibits enzymatic activity of CaN

17 μM^a

Baumgrass R 2001 [199]

INCA1

0.5 μM* ^f

Roehrl MH 2004 [114]

INCA2

disturb CaN-NFATc complex formation by covalent binding to CaN

0.12 μM* ^f

Roehrl MH 2004 [114]

INCA6

0.8 μM* ^f

Roehrl MH 2004 [114]

Kaempferol

inhibits enzymatic activity of CaN

51.3 μM^a

Wang H 2008 [94]

Lie120

inhibits enzymatic activity of CaN

5 μM^a

Klettner A 2001 [80]

NCI3

disturbs CaN-NFATc binding in cells

2 μM^c

Sieber M 2007 [113]

PD 144795

inhibits enzymatic activity of CaN

~3 μM^a

Gualberto A 1998 [109]

Roc-1

enhances rephosphorylation and nuclear export of NFATc

5~25 nM^c

Proksch P 2005 [136]

ST1959/DL111-IT

enhances nuclear export of NFATc

13.5 μM

Lindstedt R 2009 [128]

Thiopental

inhibits CaM-dependent activity of CaN

0.18 mM^a

Humar M 2004 [97]

Trifluoperazine

inhibits binding of CaM to CaN

8 μM^g

Aussel C 1995 [144]

Tropisetron

inhibits CaN-dependent NFATc transactivation

~50 μM^c

Vega Lde L 2005 [138]

UR-1505

inhibits NFATc binding to DNA

100~300 μM^h

Román J 2007 [133]

WIN 53071

alters NFATc binding to DNA

3.4 μM^h

Baine Y 1995 [141]

Inhibitors of calcineurin-dependent signalling - unknown mode of action

Caffeic Acid Phenethyl Ester

N.D.

0,1~1 μM^c

Marquez N 2003 [146]

KRM-III

N.D.

5 μM^c

Jung EJ 2009 [145]

NFAT-68

N.D.

0.63 μM^c

Burres NS 1995 [152]

YM-53792

N.D.

50 nM^c

Kuromitsu S 1997 [149]

Punicalagin

N.D.

< 5 μM^g

Lee SI 2008 [153]

Imperatorin

N.D.

37 μM^c

Marquez N 2004 [154]

Quinolone alkaloid compounds 1 and 3

N.D.

3.4 μM^c

Jin HZ 2004 [155]

Impressic acid

N.D.

12.6 μM^c

Cai XF 2004 [159]

oleanane triterpenoid compound 3

N.D.

4.6 μM^c

Dat NT 2004 [162]

Gomisin N

N.D.

1.33 μM^c

Lee IS 2003 [163]