GSK-3β Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S7193 1-Azakenpaullone

1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.

Selective GSK-3β, IC50: 18 nM
S1590 TWS119

TWS119 is a GSK-3β inhibitor with IC50 of 30 nM; capable of inducing neuronal differentiation and may be useful to stem cell biology.

Selective GSK-3β, IC50: 30 nM
S7435 AR-A014418

AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM, without significant inhibition on 26 other kinases tested.

Selective GSK-3β, Ki: 38 nM; GSK-3β, IC50: 104 nM; GSK-3β, Ki: 38 nM; GSK-3β, IC50: 104 nM; GSK-3β, Ki: 38 nM; GSK-3β, IC50: 104 nM; GSK-3β, Ki: 38 nM; GSK-3β, IC50: 104 nM; GSK-3β, Ki: 38 nM; GSK-3β, IC50: 104 nM
S7566 IM-12

IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.

Selective GSK-3β, IC50: 53 nM
S2823 Tideglusib

Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.

Selective GSK-3β, IC50: 60 nM
S2386 Indirubin

Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.

Selective GSK-3β, IC50: 0.6 μM
S2926 TDZD-8

TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.

Selective GSK-3β, IC50: 2 μM
S2745 CHIR-98014

CHIR-98014 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.

Pan GSK-3β, IC50: 0.58 nM
S7063 LY2090314

LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 2.

Pan GSK-3β, IC50: 0.9 nM
S2924 CHIR-99021 (CT99021) HCl

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; ability to distinguish between GSK-3 and its closest homologs Cdc2 and ERK2.

Pan GSK-3β, IC50: 6.7 nM
S7145 AZD1080

AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

Pan GSK-3β, IC50: 31 nM
S1075 SB216763

SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β.

Pan GSK-3β, IC50: ~34.3 nM
S2729 SB415286

SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.

Pan GSK-3β, IC50: ~78 nM