GSK-3 Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S1263	CHIR-99021 (Laduviglusib)	Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 values of 10 nM and 6.7 nM, respectively. It does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. This compound functions as a Wnt/β-catenin activator and induces autophagy.	Cancer Cell, 2025, 43(4):776-796.e14 Circulation, 2025, 151(20):1436-1448 Nat Biomed Eng, 2025, 9(1):93-108
S2924	Laduviglusib (CHIR-99021) Hydrochloride	Laduviglusib (CHIR-99021; CT99021) HCl 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. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.	Cell, 2025, 188(11):2974-2991.e20 Cell, 2025, S0092-8674(25)00807-4 Protein Cell, 2025, pwaf098
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. This compound activates autophagy.	iScience, 2025, 28(11):113642 iScience, 2025, 28(8):113117 Oncol Rep, 2025, 54(4)125
S2745	CHIR-98014	CHIR-98014 (CT98014) 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.	Med Oncol, 2025, 42(8):333 Stem Cell Res, 2025, 87:103797 Commun Med (Lond), 2025, 5(1):323
S1590	TWS119	TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; this compound is capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition by this chemical triggers autophagy.	Discov Oncol, 2025, 16(1):364 Nat Commun, 2024, 15(1):2089 Sci Rep, 2024, 14(1):5038
S7198	GSK-3 Inhibitor IX (BIO)	BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) 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 with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.	Cell Rep, 2025, 44(3):115361 Development, 2025, 152(3)DEV204214 bioRxiv, 2025, 2025.04.11.648340
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. This compound is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.	Cell Mol Gastroenterol Hepatol, 2026, 20(1):101633 Cancer Cell, 2025, 43(4):776-796.e14 Cell Rep, 2025, 44(5):115617
S2823	Tideglusib	Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; this compound fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.	Addict Biol, 2025, 30(5):e70044 Cell Rep, 2024, 43(9):114667 SLAS Discov, 2024, S2472-5552(24)00007-8
S2729	SB415286	SB415286 is a potent GSK3α inhibitor with IC50/K_i of 78 nM/31 nM with equally effective inhibition of GSK-3β. This compound causes MM cell growth arrest and apoptosis.	bioRxiv, 2025, 2025.03.08.642085 Front Immunol, 2022, 13:880988 Sci Rep, 2022, 12(1):7
S7435	AR-A014418	AR-A014418 (GSK-3β Inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor with IC50 and K_i of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.	Cancer Med, 2025, 14(5):e70047 NPJ Precis Oncol, 2024, 8(1):264 Commun Biol, 2024, 7(1):1380
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
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
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
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 Chinese Medicine, 2025, 126 Int J Mol Sci, 2023, 24(17)13593
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
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
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, 2024, 424 Antioxidants (Basel), 2024, 13(4)424 International Journal of Clinical and Experimental Medicine, 2019, 10164-10176
S7145	AZD1080	AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with K_i 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
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.
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
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
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.