| 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 |