Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Protein Kinase A (PKA; cAMP-Dependent Protein Kinase) Inhibitors, continued
Product Cat. No. Comments Size Price
Adenosine 3´,5´-cyclic
Monophosphorothioate,
2´-O-Monobutyryl-,
Rp-Isomer, Sodium Salt
4-Cyano-3methylisoquinoline
116825 (Rp-MB-cAMPS, Na)
A cell-permeable precursor of Rp-cAMPS (Cat. No. 68 4), a PKA inhibitor.
Rp-MB-cAMPS is cleaved by intracellular esterases to release butyrate and Rp-cAMPS.
The Rp-cAMPS binds to the cAMP binding site on PKA type I and type II, thereby
preventing holoenzyme dissociation and PKA activation.
238900 A potent, cell-permeable, specific inhibitor of PKA (IC 50 = 30 nM). Inhibition is
competitive with respect to ATP.
Daphnetin 268295 (7,8-Dihydroxy-2H-1-benzopyran-2-one; 7,8-Dihydroxycoumarin)
A coumarin analog that acts as an inhibitor of several protein kinases. Inhibits EGFR
kinase (IC 50 = 7.67 mM), PKA (IC 50 = 9.33 mM), and PKC (IC 50 = 25 mM), in vitro.
Ellagic Acid, Dihydrate 324683 (4,4´,5,5´,6,6´-Hexahydroxydiphenic Acid 2,6,2´,6´-Dilactone)
A potent antioxidant that acts as a potent inhibitor of PKA catalytic subunit
and PKC (IC 50 = 2 and 8 mM respectively). Also inhibits DNA topoisomerases I and II
(IC 50 = .8 mM and 2. mM, respectively).
H-7, Dihydrochloride 371955 [1-(5-Isoquinolinesulfonyl)-2-methylpiperazine, 2HCl]
A broad based serine-threonine kinase inhibitor. Potent inhibitor of MLCK (K i = 97 mM), PKA
(K i = 3.0 mM), PKC (K i = 6 mM), and PKG (K i = 5.8 mM). Not available for sale in Japan.
H-8, Dihydrochloride 371958 {N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide, 2HCl}
Highly active inhibitor of cyclic-nucleotide-dependent protein kinases. Inhibits MLCK
(K i = 68 mM), PKA (K i = .2 mM), PKC (K i = 5 mM), and PKG (K i = 480 nM). Not available
for sale in Japan.
H-9, Dihydrochloride 371961 [N-(2-Aminoethyl)-5-isoquinolinesulfonamide, 2HCl]
Closely resembles H-8 in its chemical structure and inhibition potency. Inhibits PKA
(K i = .9 mM), PKC (K i = 8 mM), and PKG (K i = 870 nM). Useful as a ligand for the
separation and purification of these three enyzmes. Not available for sale in Japan.
H-89, Dihydrochloride 371963 {N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl}
A cell-permeable, selective and potent inhibitor of PKA (K i = 48 nM). Inhibits other
kinases at several fold higher concentrations: MLCK (K i = 28.3 mM), CaM kinase II
(K i = 29.7 mM), PKC (K i = 3 .7 mM), casein kinase I (K i = 38.3 mM), and Rho Kinase II
(IC 50 = 270 nM). Not available for sale in Japan.
InSolution H-89,
Dihydrochloride
HA 004,
Dihydrochloride
HA 077,
Dihydrochloride
K-252a, Nocardiopsis
sp.
InSolution K-252a,
Nocardiopsis sp.
K-252b,
Nocardiopsis sp.
371962 {N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl}
A 0 mM ( mg/ 93 ml) solution of H-89, Dihydrochloride (Cat. No. 37 963) in
anhydrous DMSO. Not available for sale in Japan.
371964 [N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide, 2HCl]
A novel intracellular Ca 2+ -antagonist that inhibits CaM Kinase II (K i = 3 mM),
MLCK (K i = 50 mM), PKA (K i = 2.3 mM), PKC (K i = 40 mM), and PKG (K i = .3 mM).
Not available for sale in Japan.
371970 [Fasudil; (5-Isoquinolinesulfonyl)homopiperazine, 2HCl]
Cell-permeable Ca 2+ -antagonist that inhibits PKA (IC 50 = .6 mM), PKG (IC 50 = .6 mM),
and MLCK (IC 50 = 3.6 mM). Also reported to potently inhibit Rho-associated kinase.
420298 A cell-permeable inhibitor of CaM kinase II (K i = .8 nM), MLCK (K i = 7 nM), PKA
(K i = 8 nM), PKC (K i = 25 nM), and PKG (K i = 20 nM). Also acts as a potent inhibitor
(IC 50 = 3 nM) of the tyrosine protein kinase activity of the NGF receptor gp 40 trk , the
product of the trk proto-oncogene.
5 mmol $452
mg $95
0 mg $50
500 mg $57
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mg
5 mg
mg
5 mg
$84
$327
$84
$327
mg $84
mg $84
mg $84
mg $57
mg $84
00 mg $ 33
420297 A mM ( 00 mg/2 4 ml) solution of K-252a (Cat. No. 420298) in DMSO. 00 mg $ 28
420319 A non-selective inhibitor of MLCK (K i = 47 nM), PKA (K i = 90 nM), PKC (K i = 20 nM),
and PKG (K i = 00 nM).
KT5720 420320 Prepared by a chemical modification of K-252a (Cat. No. 420298). Potent specific
cell-permeable inhibitor of PKA (K i = 56 nM) that does not significantly affect the
activity of PKC, PKG, or MLCK.
InSolution KT5720 420323 A 2 mM (50 mg/47 ml) solution of KT5720 (Cat. No. 420320) in anhydrous DMSO. 50 mg $76
Piceatannol 527948 (trans-3,3´,4,5´-Tetrahydroxystilbene)
A plant metabolite that preferentially inhibits the activity of p72 Syk (IC 50 ~ 0 mM).
Also inhibits rat liver PKA catalytic subunit (IC 50 = 3 mM), PKC (IC 50 = 8 mM),
MLCK (IC 50 = 2 mM), and wheat embryo Ca 2+ /dependent protein kinase (IC 50 = 9 mM).
50 mg
00 mg
50 mg
00 mg
$76
$ 33
$76
$ 33
mg $4