GSK-3

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S2924 CHIR-99021 (CT99021) HCl <1 mg/mL 93 mg/mL 2 mg/mL
S1075 SB216763 <1 mg/mL 23 mg/mL <1 mg/mL
S2745 CHIR-98014 <1 mg/mL 8 mg/mL <1 mg/mL
S1590 TWS119 <1 mg/mL 64 mg/mL <1 mg/mL
S2823 Tideglusib <1 mg/mL 8 mg/mL <1 mg/mL
S5439 5-Bromoindole -1 mg/mL 39 mg/mL -1 mg/mL
S8696 2-D08 <1 mg/mL 54 mg/mL <1 mg/mL
S2729 SB415286 <1 mg/mL 72 mg/mL 72 mg/mL
S7198 BIO <1 mg/mL 71 mg/mL 6 mg/mL
S1263 CHIR-99021 (CT99021) <1 mg/mL 10 mg/mL <1 mg/mL
S7253 AZD2858 <1 mg/mL 7 mg/mL <1 mg/mL
S7145 AZD1080 <1 mg/mL 52 mg/mL <1 mg/mL
S7435 AR-A014418 <1 mg/mL 61 mg/mL <1 mg/mL
S2926 TDZD-8 <1 mg/mL 44.5 mg/mL 44.5 mg/mL
S7063 LY2090314 <1 mg/mL 100 mg/mL 2 mg/mL
S7566 IM-12 <1 mg/mL 75 mg/mL 10 mg/mL
S7915 BIO-acetoxime <1 mg/mL 19 mg/mL <1 mg/mL
S2386 Indirubin <1 mg/mL 53 mg/mL <1 mg/mL
S7722 Bikinin <1 mg/mL 54 mg/mL <1 mg/mL
S7193 1-Azakenpaullone <1 mg/mL 66 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S2924

CHIR-99021 (CT99021) HCl

CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.

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.

S2745

CHIR-98014

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

S1590

TWS119

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

S2823

Tideglusib

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

S5439New

5-Bromoindole

5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).

S8696New

2-D08

2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

S2729

SB415286

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

S7198

BIO

BIO is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor.

S1263

CHIR-99021 (CT99021)

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

S7253

AZD2858

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

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.

S7435

AR-A014418

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

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.

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. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.

S7566

IM-12

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

S7915

BIO-acetoxime

BIO-acetoxime is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.

S2386

Indirubin

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

S7722

Bikinin

Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.

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.

Tags: GSK-3 inhibition | GSK-3 cancer | GSK-3 signaling pathway | GSK-3 activation | GSK-3 activity | GSK-3 beta pathway | GSK-3 phosphorylation | GSK-3 beta phosphorylation | GSK-3 assay | GSK-3 inhibitor review