GSK-3

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GSK-3 Signaling Pathway Map

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GSK-3 Products

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  • New GSK-3 Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
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. Alsterpaullone 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. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
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. SB216763 activates autophagy.
Biomed Pharmacother, 2022, 145:112432
J Clin Invest, 2021, 131(6)136098
Autophagy, 2021, 1-19
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. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Cell, 2021, 184(11):2843-2859.e20
Nat Genet, 2021, 53(12):1686-1697
Nat Genet, 2021, 53(4):467-476
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. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
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. GSK-3β inhibition triggers autophagy.
Nat Commun, 2021, 12(1):4536
EMBO Rep, 2021, e51503
Cell Rep, 2021, 36(1):109311
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.
Molecules, 2021, 26(5)1210
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S2729 SB415286 SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.
Int J Biol Macromol, 2021, 180:97-111
Toxicol Lett, 2021, 341:68-79
Mol Cell, 2020, 80(6):1104-1122.e9
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.
Redox Biol, 2021, 43:101970
Mol Ther, 2021, 26(7): 1644–1659
Cancer Discov, 2021, candisc.0551.2021
S2823 Tideglusib (NP031112) Tideglusib (NP031112, NP-12) 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.
J Virol, 2021, JVI.02393-20
Adv Biol Regul, 2021, S2212-4926(20)30091-9
Mol Cell, 2020, 80(6):1104-1122.e9
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; 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.
Nat Genet, 2021, 53(12):1686-1697
Nat Genet, 2021, 53(4):467-476
Eur Heart J, 2021, ehab547
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.
Sci Transl Med, 2020, 12(554):eaba3613
FASEB J, 2018, 32(7):3924-3935
Nat Commun, 2017, 1;8(1):1232
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. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S5439 5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
S6085New 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.
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.
Cell, 2021, 184(1):243-256.e18
Mol Cell, 2021, S1097-2765(21)00735-8
Nat Commun, 2021, 12(1):2346
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
Carcinogenesis, 2020, 41(7):993-1004
Int J Mol Sci, 2020, 21(18)E6826
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.
Cancer Lett, 2020, 1;481:1-14
Carcinogenesis, 2020, 41(7):993-1004
Front Oncol, 2020, 10:565225
S7198 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.
Mol Cell, 2021, 81(18):3803-3819.e7
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Front Cell Dev Biol, 2021, 9:662868
S7253 AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
J Biol Chem, 2021, S0021-9258(21)00485-3
Carcinogenesis, 2020, 41(7):993-1004
Elife, 2019, 10.7554/eLife.42274
S7435 AR-A014418 AR-A014418 (GSK-3β Inhibitor VIII) 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.
J Med Chem, 2021, 64(11):7483-7506
FEBS J, 2021, 10.1111/febs.15898
Oncol Lett, 2021, 21(4):269
S7566 IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
Proc Natl Acad Sci U S A, 2020, 117(44):27435-27444
Carcinogenesis, 2020, 41(7):993-1004
Anat Rec (Hoboken), 2020, 303(9):2344-2356
S7722 Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
Plant Cell, 2021, koab137
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.
Cancer Cell, 2017, 32(6):748-760
J Funct Foods, 2017, 10.1016/j.jff.2017.01.040
Journal of Functional Foods, 2017, 31:217-228
S7954 CP21R7 (CP21) CP21R7 (CP21) is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
ACS Nano, 2021, 10.1021/acsnano.1c06452
Sci Adv, 2020, 6(30):eaba7606
Front Cell Dev Biol, 2020, 15;8:309
S8696 2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-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.
Nat Commun, 2021, 12(1):4794
Cancers (Basel), 2021, 13(14)3475
Cancer Sci, 2021, 112(10):4075-4086
S9602 9-ing-41 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.
S9638New 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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).
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.
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
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. Alsterpaullone 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. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
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. SB216763 activates autophagy.
Biomed Pharmacother, 2022, 145:112432
J Clin Invest, 2021, 131(6)136098
Autophagy, 2021, 1-19
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. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Cell, 2021, 184(11):2843-2859.e20
Nat Genet, 2021, 53(12):1686-1697
Nat Genet, 2021, 53(4):467-476
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. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
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. GSK-3β inhibition triggers autophagy.
Nat Commun, 2021, 12(1):4536
EMBO Rep, 2021, e51503
Cell Rep, 2021, 36(1):109311
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.
Molecules, 2021, 26(5)1210
Carcinogenesis, 2020, 41(7):993-1004
J Med Virol, 2019, 91(8):1440-1447
S2729 SB415286 SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.
Int J Biol Macromol, 2021, 180:97-111
Toxicol Lett, 2021, 341:68-79
Mol Cell, 2020, 80(6):1104-1122.e9
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.
Redox Biol, 2021, 43:101970
Mol Ther, 2021, 26(7): 1644–1659
Cancer Discov, 2021, candisc.0551.2021
S2823 Tideglusib (NP031112) Tideglusib (NP031112, NP-12) 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.
J Virol, 2021, JVI.02393-20
Adv Biol Regul, 2021, S2212-4926(20)30091-9
Mol Cell, 2020, 80(6):1104-1122.e9
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; 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.
Nat Genet, 2021, 53(12):1686-1697
Nat Genet, 2021, 53(4):467-476
Eur Heart J, 2021, ehab547
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.
Sci Transl Med, 2020, 12(554):eaba3613
FASEB J, 2018, 32(7):3924-3935
Nat Commun, 2017, 1;8(1):1232
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. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S5439 5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
S6085New 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.
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.
Cell, 2021, 184(1):243-256.e18
Mol Cell, 2021, S1097-2765(21)00735-8
Nat Commun, 2021, 12(1):2346
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
Carcinogenesis, 2020, 41(7):993-1004
Int J Mol Sci, 2020, 21(18)E6826
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.
Cancer Lett, 2020, 1;481:1-14
Carcinogenesis, 2020, 41(7):993-1004
Front Oncol, 2020, 10:565225
S7198 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.
Mol Cell, 2021, 81(18):3803-3819.e7
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Front Cell Dev Biol, 2021, 9:662868
S7253 AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
J Biol Chem, 2021, S0021-9258(21)00485-3
Carcinogenesis, 2020, 41(7):993-1004
Elife, 2019, 10.7554/eLife.42274
S7435 AR-A014418 AR-A014418 (GSK-3β Inhibitor VIII) 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.
J Med Chem, 2021, 64(11):7483-7506
FEBS J, 2021, 10.1111/febs.15898
Oncol Lett, 2021, 21(4):269
S7566 IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
Proc Natl Acad Sci U S A, 2020, 117(44):27435-27444
Carcinogenesis, 2020, 41(7):993-1004
Anat Rec (Hoboken), 2020, 303(9):2344-2356
S7722 Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
Plant Cell, 2021, koab137
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.
Cancer Cell, 2017, 32(6):748-760
J Funct Foods, 2017, 10.1016/j.jff.2017.01.040
Journal of Functional Foods, 2017, 31:217-228
S7954 CP21R7 (CP21) CP21R7 (CP21) is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
ACS Nano, 2021, 10.1021/acsnano.1c06452
Sci Adv, 2020, 6(30):eaba7606
Front Cell Dev Biol, 2020, 15;8:309
S8696 2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-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.
Nat Commun, 2021, 12(1):4794
Cancers (Basel), 2021, 13(14)3475
Cancer Sci, 2021, 112(10):4075-4086
S9602 9-ing-41 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.
S9638New 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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).
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.
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S6085New 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.
S9638New 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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).
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