Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Glycogen Synthase Kinase Inhibitors, continued
Product Cat. No. Comments Size Price
Cdk /5 Inhibitor 217720 (3-Amino-1H-pyrazolo[3,4-b]quinoxaline)
A pyrazoloquinoxaline compound that effectively inhibits Cdk /B, Cdk 5/p25, and
GSK-3b (IC 50 = 0.6 mM, 0.4 mM, and mM respectively).
GSK-3b Inhibitor I 361540 (TDZD-8; 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione)
A thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP competitive
inhibitor of GSK-3b (IC 50 = 2 mM). Proposed to bind to the active site of GSK-3b.
GSK-3b Inhibitor II 361541 {Glycogen Synthase Kinase-3b Inhibitor II; 2-Thio(3-iodobenzyl)-5-(1-pyridyl)-
[1,3,4]-oxadiazole}
A 2-thio-[ ,3,4]-oxadiazole-pyridyl derivative that acts as a potent inhibitor of GSK-3b
(IC 50 = 390 nM).
GSK-3b Inhibitor III 361542 (2,4-Dibenzyl-5-oxothiadiazolidine-3-thione; OTDZT)
An oxothiadiazolidine-3-thione analog that acts as a non-ATP competitive inhibitor of
GSK-3b (IC 50 = 0 mM).
N GSK-3b Inhibitor VI 361547 [2-Chloro-1-(4,5-dibromo-thiophen-2-yl)-ethanone]
A thienyl a-chloromethyl ketone compound that acts as a cell-permeable, irreversible,
and non-ATP competitive inhibitor of GSK-3b (IC 50 = mM). This reactive alkylating
agent is selective towards GSK-3b and does not affect PKA activity even at
concentrations as high as 00 mM.
GSK-3b Inhibitor VII 361548 (a-4-Dibromoacetophenone; Tau Protein Kinase I Inhibitor; TPK I Inhibitor)
A cell-permeable, selective, irreversible, and non-ATP competitive inhibitor of GSK-3b
(IC 50 = 500 nM).
GSK-3b Inhibitor VIII 361549 [AR-A014418; N-(4-Methoxybenzyl)-N´-(5-nitro-1,3-thiazol-2-yl)urea]
A cell-permeable, potent, and highly specific inhibitor of glycogen synthase kinase-3b
(GSK-3b) (IC 50 = 04 nM). Inhibition is competitive with respect to ATP (K i = 38 nM).
N InSolution GSK-3b
Inhibitor VIII
5 mg $ 8
5 mg $83
5 mg $89
mg $62
5 mg $95
5 mg $84
5 mg $84
361557 A 25 mM (5 mg/649 ml) solution of GSK-3b Inhibitor VIII (Cat. No. 36 549) in DMSO. 5 mg $84
GSK-3 Inhibitor IX 361550 [BIO; (2´Z,3´E)-6-Bromoindirubin-3´-oxime]
A cell-permeable, highly potent, selective, reversible, and ATP-competitive
inhibitor of GSK-3a/b (IC 50 = 5 nM). At higher concentrations, inhibits Cdk2/cyclin A
(IC 50 = 300 nM) and Cdk5/p25 (IC 50 = 83 nM).
N InSolution GSK-3
Inhibitor IX
mg $95
361552 A 0 mM (500 mg/ 40 ml) solution of GSK-3 Inhibitor IX (Cat. No. 36 550) in DMSO. 500 mg $63
N GSK-3 Inhibitor X 361551 [BIO-Acetoxime; (2´Z,3´E)-6-Bromoindirubin-3´-acetoxime]
An acetoxime analog of BIO (GSK-3 Inhibitor IX, Cat. No. 36 550) that exhibits greater
selectivity for GSK-3a/b (IC 50 = 0 nM) over Cdk5/p25, Cdk2/A, and Cdk /B
(IC 50 = 2.4 mM, 4.3 mM, and 63 mM, respectively).
N GSK-3b Inhibitor XI 361553 {3-(1-(3-Hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-pyrazin-2-yl-pyrrole-2,
5-dione}
N GSK-3b Inhibitor XII,
TWS 9
A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and
ATP-competitive inhibitor of GSK-3b (K i = 25 nM) and minimally inhibits a panel of 79
commonly studied protein kinases, including several PKC isozymes. Shown to increase
intracellular glycogen synthase activity in HEK293 cells with an EC 50 of 32 nM and
demonstrate metabolic stability in human liver microsomes (HLM; t /2 > 00 min).
361554 (Neurogenesis Inducer, TWS119)
A cell-permeable pyrrolopyrimidine compound that acts as a potent and selective
inhibitor of GSK-3b (IC 50 = 30 nM). Binds to GSK-3b with high-affinity (K d = 26 nM)
and increases the level of b-catenin, a downstream substrate of GSK-3b in the Wnt
signaling pathway.
N GSK-3 Inhibitor XIII 361555 [(5-Methyl-1H-pyrazol-3-yl)-(2-phenylquinazolin-4-yl)amine]
An aminopyrazole compound that acts as a potent and ATP-binding site inhibitor
of GSK-3 with a K i of 24 nM.
N GSK-3 Inhibitor XIV,
Control, MeBIO
361556 (1-Methyl-BIO)
A cell-permeable N-methylated analog of GSK-3 Inhibitor IX, BIO (Cat. No. 36 550)
that serves as a relevant kinase inactive control (IC 50 > 92 mM for Cdk /B, and > 00 mM
for Cdk5/p25 and GSK-3a/b).
mg $95
mg $ 32
20 Orders Phone 800 854 34 7
Calbiochem • Inhibitor SourceBook
Fax 800 776 0999
Web www.emdbiosciences.com/calbiochem
mg
5 mg
mg
5 mg
$90
$278
$67
$20
mg $93