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GSK-3 Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7566 IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and this compound also enhances canonical Wnt signalling.
Front Pharmacol, 2025, 16:1496511
Discov Oncol, 2025, 16(1):901
Nat Commun, 2024, 15(1):668
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S7193 1-Azakenpaullone 1-Azakenpaullone (1-Akp) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.
Environ Int, 2025, 204:109820
EMBO Rep, 2024, 25(5):2188-2201
Exp Neurol, 2023, 359:114233
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S7954 CP21R7 CP21R7 is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
Am J Transl Res, 2025, 17(10):8060-8075
J Nanobiotechnology, 2024, 22(1):373
iScience, 2024, 27(10):110862
S2386 Indirubin (NSC 105327) Indirubin (NSC 105327) is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.
Front Oncol, 2025, 15:1486671
iScience, 2024, 27(10):110862
BMC Complement Med Ther, 2024, 24(1):28
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S2926 TDZD-8 TDZD-8 (NP 01139) 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.
Chin Med, 2025, 20(1):126
Int J Mol Sci, 2023, 24(17)13593
PLoS One, 2023, 18(4):e0284332
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S7253 AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
Environ Mol Mutagen, 2024, 10.1002/em.22604
Sci Rep, 2022, 12(1):7
J Biol Chem, 2021, S0021-9258(21)00485-3
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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.
Oncogene, 2020, 39(20):4132-4154
Int J Mol Sci, 2020, 21(18)E6826
Carcinogenesis, 2020, 41(7):993-1004
S7915 BIO-acetoxime BIO-acetoxime (GSK-3 Inhibitor X) 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.
Antioxidants (Basel), 2024, 13(4)424
Cancer Cell, 2017, 32(6):748-760
J Funct Foods, 2017, 10.1016/j.jff.2017.01.040
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S7722 Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
Cell Rep, 2025, 44(4):115569
Cell Rep, 2023, 42(3):112187
Plant Physiol, 2022, kiac015
E3092 Paeoniae Radix Rubra Extract Paeoniae Radix Rubra Extract is obtained from Paeoniae Radix Rubra, prevents deep vein thrombosis by ameliorating inflammation through inhibiting GSK3β activity.
E0381 (E/Z)-GSK-3β inhibitor 1 (E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers, in which GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor with an IC50 of 4.19 nM.
E2819 PF-04802367 PF-04802367 (PF-367) is a highly selective Glycogen synthase kinase-3 (GSK-3) inhibitor with IC50s of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay.
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. This compound also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. It activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S5439 5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
S6085 KY19382 (A3051) KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively.
E4674 Cu(II)GTSM Cu(II)GTSM is a potent cell-permeable inhibitor of GSK3β that also inhibits Aβ oligomers and reduces tau phosphorylation. It shows potential as an anticancer and antimicrobial agent and may restore cognitive function by inhibiting neurotoxic Aβ trimers and phosphorylated tau.
S9602 Elraglusib Elraglusib(9-ING-41) is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with antitumor activity. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β.
E0798 WAY-119064 WAY-119064 is a potent glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 value of 80.5 nM.
S9156 Chonglou Saponin VII Chonglou Saponin VII (Dioscinin, Polyphyllin-VII, Paris saponin-VII), a kind of steroidal saponins from Chonglou (Rhizoma Paridis Chonglou), inhibits EMT and reduces the invasion of ovarian cancer cells via the GSK-3β/β-catenin signaling pathway.
S9638 BRD0705 BRD0705 is a potent, paralog selective and orally active inhibitor of GSK3α (Glycogen synthase kinase 3α) with IC50 of 66 nM and Kd of 4.8 μM. This compound also inhibits GSK3β with IC50 of 515 nM. It can be used for acute myeloid leukemia (AML).
E7201 Ceftriaxone Ceftriaxone is a long-acting, broad-spectrum β-lactam, third-generation semisynthetic cephalosporin with broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and some anaerobic bacteria. It also acts as a covalent inhibitor of GSK3β with an IC50 of 0.78 μM after 60 minutes of preincubation with the enzyme in vitro.
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. This compound also decrease GSK3β phosphorylation. It induces apoptosis. Phase 2.
Nat Struct Mol Biol, 2025, 10.1038/s41594-025-01517-5
Cell Rep Med, 2025, S2666-3791(25)00231-9
Nat Commun, 2024, 15(1):10028
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S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. This compound exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. It induces apoptosis and caspase-3 and caspase-8 activity. This chemical increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
bioRxiv, 2025, 2025.07.17.665404
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
S0765 MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
Sci Rep, 2025, 15(1):1283
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. This compound also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. It induces apoptosis by activation of caspase-9. This chemical has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
Cell Mol Life Sci, 2025, 82(1):311
E0474 7BIO 7-bromoindirubin-3-oxime (7BIO), an indirubin derivative derived from indirubin-3-oxime, possesses inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β), also potently inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, and activation of astrocytes and microglia.
E5780 Laduviglusib trihydrochloride Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. This compound shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. It is also a potent Wnt/β-catenin signaling pathway activator. This chemical enhances mouse and human embryonic stem cells self-renewal. It induces autophagy.
E2821 RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
E7732 GNF4877 GNF4877 is an aminopyrazine and a potent inhibitor of GSK3β and DYRK1A with an IC50 of 16 nM and 6 nM, respectively. It blocks nuclear factor of activated T-cells (NFATc) nuclear export, promotes β-cell proliferation, and is useful for research on diabetes drug development.