Information
X


Glycogen Synthase Kinase Inhibitors

Related Resources
Merck:/topic/images/Biosciences/BIOL_321sm_M.jpg
Merck:/topic/images/Biosciences/gskpathway_thumb.jpg

Glycogen Synthase Kinase-3b (GSK-3b), a highly conserved, ubiquitously expressed serine/threonine protein kinase, is involved in the signal transduction cascades of multiple cellular processes. It is negatively regulated by protein kinase B/Akt and by the Wnt signaling pathway. Higher levels of GSK-3b have been shown in pre-tangle and in phosphorylated tau-bearing neurons. Overexpression of GSK-3b is a characteristic feature of Alzheimer's disease. GSK-3b accounts for most major phosphorylation sites of fetal and paired helical filament-tau. b-Amyloid peptides are shown to activate GSK-3b, suggesting that activation of GSK-3b is a key mechanism in pathogenesis of Alzheimer's disease. The development of GSK-3 inhibitors holds considerable promise for reducing tau phosphorylation and debilitating effects of Alzheimer's disease.

InhibitorSelect™ 96-Well Protein Kinase Inhibitor Library II (Cat. No. 539745)
Consists of 80, well-characterized, cell permeable, potent and reversible protein kinase inhibitors; the majority of which are ATP-competitive. They are supplied in a convenient 96-well plate format at a concentration of 10 mM in DMSO.
InhibitorSelect™ 384-Well Protein Kinase Inhibitor Library I (Cat. No. 539743)
Consists of 160 well-characterized, cell-permeable, potent, and reversible protein kinase inhibitors; the majority of which are ATP-competitive. They are supplied in a convenient 384-well plate format at a concentration of 10 mM in DMSO.
Aloisine, RP106 (Cat. No. 128135)
A cell-permeable, potent, selective ATP-competitive inhibitor of Cdk1/cyclin B (IC50 = 700 nM), Cdk5/p25 (IC50 = 1.5 mM), and GSK-3 (IC50 = 920 nM).
Aloisine A (Cat. No. 128125)
Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM and 1.5 µM for GSK-3a, GSK-3b, respectively), and c-Jun N-terminal kinase (JNK; IC50 ~ 3 - 10 µM).
Alsterpaullone (Cat. No. 126870)
A potent inhibitor of Cdk1/cyclin B (IC50 = 35 nM). Displays remarkable in vitro antitumor activity. Inhibits Tau phosphorylation at sites that are typically phosphorylated by GSK-3b in Alzheimer’s disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.
Cdk1/5 Inhibitor (Cat. No. 217720)
A 3-amino substituted pyrazoloquinoxaline compound that acts as a selective inhibitor of cyclin-dependent kinases 1 and 5 (Cdks; IC50 = 0.6 µM and 0.4 µM for Cdk1/cyclin B and Cdk5/p25, respectively). Also shown to inhibit GSK-3b with (IC50 = 1 µM).
Cdc7/Cdk9 Inhibitor (Cat. No. 217707)
A cell-permeable pyrrolopyridinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 (IC50 = 10 and 34 nM, respectively) with good selectivity over a panel of 31 other kinases, including GSK-3b, Cdk2, Cdk1, Cdk5, MK-2, Plk1, and Chk2 (IC50 = 0.22, 0.24, 0.25, 0.46, 0.47, 0.98, and 1.1 µM, respectively).
FRATtide (Cat. No. 344265)
A peptide corresponding to amino acids 188 - 226 of FRAT1 (frequently rearranged in advanced T-cell lymphomas 1), a mammalian homolog of GSK-3 binding protein. Binds to the C-terminal lobe of GSK-3 and prevents the binding of “unprimed” substrates such as axin, b-catenin and tau. Exhibits little effect on GSK-3 catalyzed phosphorylation of “primed” (pre-phosphorylated) substrates such as glycogen synthase and eIF2B.
GSK-3 Inhibitor IX in Solution (Cat. No. 361552)
Supplied as a 10 mM (500 mg/140 ml) solution of GSK-3 Inhibitor IX (Cat. No. 361550) in DMSO.
GSK-3 Inhibitor X (Cat No. 361551)
An acetoxime analog of BIO, GSK-3 Inhibitor IX (Cat. No. 361550) that exhibits greater selectivity for GSK-3a/b (IC50 = 0.01 mM) over CDK5/p25, CDK2/A and CDK1/B (IC50 = 2.4 mM, 4.3 mM and 63 mM, respectively).
GSK-3 Inhibitor XIII (Cat. No. 361555)
An aminopyrazole compound that acts as a potent and ATP-binding site inhibitor of GSK-3 with a Ki of 24 nM.
GSK-3 Inhibitor XIV, Control, MeBIO (Cat. No. 361556)
A cell-permeable N-methylated analog of GSK-3 Inhibitor IX, BIO (Cat. No. 361550) that serves as a relevant kinase inactive control (IC50 > 92 mM for Cdk1/B, and > 100 mM for Cdk5/p25 and GSK-3a/b).
GSK-3 Inhibitor XV (Cat. No. 361558)
A cell-permeable pyridocarbazolo-cyclopentadienyl Ruthenium complex that acts as a potent, reversible and ATP-competitive inhibitor of GSK-3 (IC50 = 0.7 nM and 1.1 nM for GSK-3a and GSK-3b, respectively) with moderate selectivity over PIM-1 kinase (IC50 = 6 nM). Its (R)-enantiomer (IC50 = 350 pM, 550 PM and 35 nM for GSK-3a, GSK-3b and PIM-1 kinase, respectively) is shown to increase the levels of b-Catenin and activate Wnt pathway in HEK293OT and 1205Lu melanoma cells at 25 nM, and induce a phenotype change in Zebrafish embryo at 1 mM.
GSK-3b Inhibitor I (Cat. No. 361540)
A thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP competitive inhibitor of GSK-3b (IC50 = 2 mM). Proposed to bind to the active site of GSK-3b.K; IC50 ~ 3 - 10 µM).
GSK-3b Inhibitor II (Cat. No. 361541)
A 2-thio-[1,3,4]-oxadiazole-pyridyl derivative that acts as a potent inhibitor of GSK-3b (IC50 = 390 nM).
GSK-3b Inhibitor III (Cat. No. 361542)
An oxothiadiazolidine-3-thione analog that acts as a non-ATP competitive inhibitor of GSK-3b (IC50 = 10 mM).
GSK-3b Inhibitor VI (Cat. No. 361547)
A thienyl a-chloromethyl ketone compound that acts as a cell-permeable, irreversible, and non-ATP competitive inhibitor of GSK-3b (IC50 = 1 mM). This reactive alkylating agent is selective towards GSK-3b and does not affect PKA activity even at concentrations as high as 100 mM.
GSK-3b Inhibitor VII (Cat. No. 361548)
A cell-permeable, selective, irreversible, and non-ATP competitive inhibitor of GSK-3b (IC50 = 500 nM).
GSK-3b Inhibitor VIII (Cat. No. 361549)
A cell-permeable, potent, and highly specific inhibitor of glycogen synthase kinase-3b (GSK-3b) (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM).
InSolution™ GSK-3b Inhibitor VIII (Cat. No. 361557)
A 25 mM (5 mg/649 µl) solution of GSK-3b Inhibitor VIII (Cat. No. 361549) in DMSO.
GSK-3b Inhibitor IX (Cat. No. 361550)
A cell-permeable, highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3a/b (IC50 = 5 nM). At higher concentrations, inhibits Cdk2/cyclin A (IC50 = 300 nM) and Cdk5/p25 (IC50 = 83 nM).
InSolution™ GSK-3b Inhibitor IX (Cat. No. 361552)
A 10 mM (500 µg/140 µl) solution of GSK-3 Inhibitor IX (Cat. No. 361550) in DMSO.
GSK-3b Inhibitor XI (Cat No. 361553)
A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3b (Ki = 25 nM) and minimally inhibits a panel of 79 commonly studied protein kinases, including several PKC isozymes.
GSK-3b Inhibitor XII, TWS119 (Cat. No. 361554)
A cell-permeable pyrrolopyrimidine compound that acts as a potent and selective inhibitor of GSK-3b (IC50 = 30 nM).
GSK-3b Peptide Inhibitor (Cat. No. 361545)
A phosphorylated peptide that acts as a substrate-specific, competitive inhibitor of GSK-3b (IC50 = 150 mM). At 200 mM, weakly inhibits the activities of Cdc2, CK-2, MAPK, PKA, PKB, and PKCd.
GSK-3b Peptide Inhibitor, Cell-Permeable (Cat. No. 361546)
A cell-permeable, myristoylated form of GSK-3b Peptide Inhibitor (Cat. No. 361545) with a glycine spacer. Acts as a selective, substrate-specific, competitive inhibitor of GSK-3b (IC50 = 40 mM). Does not affect the activities of Cdc2, PKB, or PKC.
Indirubin-3'-monoxime (Cat. No. 402085)
A potent cell-permeable inhibitor of GSK-3b (IC50 = 190 nM) and cyclin-dependent kinases (IC50 = 180 nM for Cdk1).
Indirubin-3'-monoxime, 5-Iodo- (Cat. No. 402086)
A highly potent, cell-permeable inhibitor of GSK-3b (IC50 = 9 nM). Reported to inhibit GSK-3b phosphorylation of human tau protein in vitro (IC50 ~100 nM) and in cells (effective concentration = 20 mM). Also inhibits Cdk1 (IC50 = 25 nM) and Cdk5 (IC50 = 20 nM).
Indirubin-3'-monoxime-5-sulfonic Acid (Cat. No. 402088)
A highly potent, selective, ATP competitive inhibitor of Cdks 1 and 5 (IC50 = 5 nM for Cdk1; IC50 = 7 nM for Cdk5). Also acts as a potent inhibitor of GSK-3b (IC50 = 80 nM).
Kenpaullone (Cat. No. 422000)
A potent, cell-permeable, ATP competitive inhibitor of GSK-3b (IC50 = 230 nM), Lck (IC50 = 470 nM) and Cdks. Inhibits Cdk1/cyclin B (IC50 = 400 nM), CdK2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 mM), and Cdk5/p25 (IC50 = 850 nM).

 

© Merck KGaA, Darmstadt, Germany, 2014


x

Welcome to Merck Millipore

 

Europe, Middle East and Africa Asia / Pacific North America, Central America and the Caribbean South America

Please choose your country:

North America, Central America and the Caribbean

South America

Europe, Middle East and Africa

Asia / Pacific

All countries from A to Z

If you can't find your country please click here.

 

Privacy Statement

 

x

Merck Chemicals Cart ()

You are entering the Millipore online shop. Both carts are maintained for you while you shop between sites. We recommend to complete your Merck order before visiting Millipore.com.

Go to Millipore Proceed to checkout


What kind of products are you looking for?

Millipore

Bio manufacturing and Life science.

Merck Chemicals

High-quality industrial and laboratory chemicals.


Important message


It is currently not possible to order Bioscience products together with other Merck products. We recommend completing your current order first.

Do you wish to proceed without completing your current order? If so, this will empty your shopping cart.