Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Protein Kinase C (PKC) Inhibitors, continued
Product Cat. No. Comments Size Price
Chelerythrine Chloride 220285 Naturally occurring alkaloid. Cell-permeable, selective inhibitor of PKC (IC 50 = 660 nM).
Acts on the catalytic domain irrespective of the attachment of the regulatory domain.
A competitive inhibitor with respect to the phosphate acceptor and a non-competitive
inhibitor with respect to ATP. Over ten-fold more potent than H-7, Dihydrochloride
(Cat. No. 37 955).
Dequalinium Chloride 263225 (DECA)
An antitumor agent and PKC inhibitor. When exposed to UV light, DECA covalently and
irreversibly inhibits PKC a or PKC b (IC 50 = 7- 8 mM).
Ellagic Acid, Dihydrate 324683 (4,4´,5,5´,6,6´-Hexahydroxydiphenic Acid 2,6,2´,6´-Dilactone)
A potent antioxidant with anti-mutagenic and anti-carcinogenic properties. Inhibits
DNA topoisomerases I and II (IC 50 = .8 mM and 2. mM, respectively). Acts as a potent
inhibitor of PKA catalytic subunit and PKC (IC 50 = 2 mM and 8 mM respectively).
Gö 6976 365250 [12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)
pyrrolo (3,4-c)-carbazole; Go 6976]
An inhibitor of PKC (IC 50 = 7.9 nM for rat brain). Selectively inhibits Ca 2+ -dependent PKC
a-isozyme (IC 50 = 2.3 nM) and PKC bI (IC 50 = 6.2 nM). Does not affect the kinase activity
of the Ca 2+ -independent PKC d , PKC e , and PKC z isoenzymes even at micromolar levels.
InSolution Gö 6976 365253 [12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)
pyrrolo (3,4-c)-carbazole; Go 6976, Solution]
A 500 mg/ml solution of Gö 6976 (Cat. No. 365250) in anhydrous DMSO.
Gö 6983 365251 {2-[1-(3-Dimethylaminopropyl)-5-methoxyindol-3-yl]-3-(1H-indol-3-yl) maleimide;
Go 6983}
A potent inhibitor of PKC that has been shown to selectively inhibit several PKC isozymes
(IC 50 = 7 nM for PKC a and PKC b ; 6 nM for PKC g ; 0 nM for PKC d ; 60 nM for PKC z ).
Gö 6983 does not effectively inhibit PKC m (IC 50 = 20 mM) and can thus be used
to differentiate PKC m from other PKC isozymes.
Gö 7874, Hydrochloride 365252 A potent and selective inhibitor of rat brain PKC (IC 50 = 4 nM) versus MLCK
(IC 50 = 20 nM), PKA (IC 50 = 50 nM), and PKG (IC 50 = 4.8 mM).
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 mM), PKC (K i = 6 mM), and PKG (K i = 5.8 mM). Not available for sale in Japan.
Iso-H-7,
Dihydrochloride
371956 [1-(5-Isoquinolinesulfonyl)-3-methylpiperazine, 2HCl]
Less potent than H-7 in inhibiting rat brain PKC isoforms (IC 50 = 50 mM).
Also inhibits other cyclic-nucleotide-dependent protein kinases.
HBDDE 372770 (2,2´,3,3´,4,4´-Hexahydroxy-1,1´-biphenyl-6,6´-dimethanol Dimethyl Ether)
An inhibitor of PKC that selectively inhibits PKC a (IC 50 = 43 mM) and PKC g (IC 50 = 50 mM)
over PKC d , PKC bI , and PKC bII isozymes.
Hispidin 377980 [6-(3,4-Dihydroxystyrl)-4-hydroxy-2-pyrone]
A potent inhibitor of PKC b isoform (IC 50 = 2 mM).
Hypericin 400076 A polycyclic dione that inhibits PKC (IC 50 = 3.3 mM). Also known to inhibit the
protein tyrosine kinase activities of the insulin receptor (IC 50 = 20 - 29 nM), EGFR
(IC 50 = 35 nM), casein kinase II (IC 50 = 6 nM), and MAP kinase (IC 50 = 4 nM).
Useful probe for PKC due to its bright red fluorescence emission and photostability.
K-252a, Nocardiopsis
sp.
InSolution K-252a,
Nocardiopsis sp.
K-252b, Nocardiopsis
sp.
420298 A cell-permeable protein kinase inhibitor that inhibits 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).
5 mg $97
500 mg $57
500 mg $57
500 mg $ 22
ml $ 36
500 mg $89
500 mg $ 00
38 Orders Phone 800 854 34 7
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mg
5 mg
$84
$327
mg $87
mg $ 38
2 mg $ 44
mg $ 05
00 mg $ 33
420297 A mM ( 00 mg/2 4 ml) solution of K-252a (Cat. No. 420298) in anhydrous 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).
K-252c 420305 Inhibits PKA (IC 50 = 25.7 mM) and PKC (IC 50 = 2.45 mM). mg $ 50
Melittin 444605 A 26-residue polypeptide from bee venom that binds calmodulin in a Ca 2+ -dependent
manner. Activates phospholipase A 2 and inhibits protein kinase C (IC 50 = 5-7 mM) by
binding to the catalytic domain in a Mg 2+ -ATP sensitive manner. Has also been used
for affinity purification of several Ca 2+ -binding proteins. A stimulator of G i a and G a
activity that is reported to inhibit adenylate cyclase activity in synaptic membranes.
50 mg
00 mg
$76
$ 33
250 mg $67