GSK-3

亜型選択性的な製品

シグナル伝達経路

GSK-3シグナル伝達経路

GSK-3製品

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  • GSK-3阻害剤 (32)
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S1263 Laduviglusib (CHIR-99021) ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S2924 Laduviglusib (CHIR-99021) HCl ラドゥビグルシブ塩酸塩 (Laduviglusib (CHIR-99021; CT99021) HCl) は CHIR-99021 の塩酸塩で、GSK-3α/β 阻害剤 (IC50 = 10 nM/6.7 nM) です。 CHIR-99021 は、最も近縁なホモログである Cdc2 および ERK2 と比較して、GSK-3 に対して 500 倍を超える選択性を示します。 CHIR-99021 は、Wnt/β-カテニン シグナル伝達経路の強力な薬理学的活性化因子です。 CHIR-99021 は、光誘発されるオートファジー (autophagy) を大幅にレスキューし、GR、RORα、およびオートファジー関連タンパク質量を増大します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
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.
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
Cell Death Dis, 2023, 14(8):500
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 decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
J Cell Biol, 2022, 221-11e202202100
Cell Death Discov, 2022, 8(1):139
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.
Sci Rep, 2024, 14(1):5038
Stem Cells Transl Med, 2023, szad085
J Nanobiotechnology, 2022, 20(1):148
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.
Cell Mol Life Sci, 2024, 81(1):92
Oncogene, 2024, 43(6):406-419
Adv Sci (Weinh), 2023, 10(12):e2206542
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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.
Commun Biol, 2023, 6(1):680
Commun Biol, 2023, 6(1):680
Cell, 2021, 184(1):243-256.e18
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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Cell, 2022, 185(22):4135-4152.e22
Int J Mol Med, 2022, 49(6)84
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.
Front Immunol, 2022, 13:880988
Sci Rep, 2022, 12(1):7
Int J Biol Macromol, 2021, 180:97-111
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.
Sci Rep, 2022, 12(1):7
J Med Chem, 2021, 64(11):7483-7506
FEBS J, 2021, 10.1111/febs.15898
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.
Exp Neurol, 2023, 359:114233
Nature, 2022, 10.1038/s41586-022-04967-9
Mol Ther Nucleic Acids, 2022, 27:147-164
S7566 IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
Nat Commun, 2024, 15(1):668
Cell Stem Cell, 2023, 30(9):1235-1245.e6
Cell Rep, 2022, 38(9):110457
S7954 CP21R7 CP21R7 is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
Cell, 2022, 185(14):2523-2541.e30
Sci Rep, 2022, 12(1):7
ACS Nano, 2021, 10.1021/acsnano.1c06452
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.
Int J Mol Sci, 2023, 24(17)13593
PLoS One, 2023, 18(4):e0284332
J Cell Mol Med, 2022, 26(14):3965-3976
S7253 AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
Sci Rep, 2022, 12(1):7
J Biol Chem, 2021, S0021-9258(21)00485-3
Carcinogenesis, 2020, 41(7):993-1004
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.
BMC Complement Med Ther, 2024, 24(1):28
EMBO Mol Med, 2022, 14(12):e15677
Sci Rep, 2022, 12(1):7
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.
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
S7722 Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
Cell Rep, 2023, 42(3):112187
Plant Physiol, 2022, kiac015
Plant Cell, 2021, koab137
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
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.
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.
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.
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.
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.
E0072 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.
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.
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. BRD0705 also inhibits GSK3β with IC50 of 515 nM. BRD0705 can be used for acute myeloid leukemia (AML).
S1263 Laduviglusib (CHIR-99021) ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S2924 Laduviglusib (CHIR-99021) HCl ラドゥビグルシブ塩酸塩 (Laduviglusib (CHIR-99021; CT99021) HCl) は CHIR-99021 の塩酸塩で、GSK-3α/β 阻害剤 (IC50 = 10 nM/6.7 nM) です。 CHIR-99021 は、最も近縁なホモログである Cdc2 および ERK2 と比較して、GSK-3 に対して 500 倍を超える選択性を示します。 CHIR-99021 は、Wnt/β-カテニン シグナル伝達経路の強力な薬理学的活性化因子です。 CHIR-99021 は、光誘発されるオートファジー (autophagy) を大幅にレスキューし、GR、RORα、およびオートファジー関連タンパク質量を増大します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
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.
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
Cell Death Dis, 2023, 14(8):500
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 decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
J Cell Biol, 2022, 221-11e202202100
Cell Death Discov, 2022, 8(1):139
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.
Sci Rep, 2024, 14(1):5038
Stem Cells Transl Med, 2023, szad085
J Nanobiotechnology, 2022, 20(1):148
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.
Cell Mol Life Sci, 2024, 81(1):92
Oncogene, 2024, 43(6):406-419
Adv Sci (Weinh), 2023, 10(12):e2206542
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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.
Commun Biol, 2023, 6(1):680
Commun Biol, 2023, 6(1):680
Cell, 2021, 184(1):243-256.e18
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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Cell, 2022, 185(22):4135-4152.e22
Int J Mol Med, 2022, 49(6)84
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.
Front Immunol, 2022, 13:880988
Sci Rep, 2022, 12(1):7
Int J Biol Macromol, 2021, 180:97-111
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.
Sci Rep, 2022, 12(1):7
J Med Chem, 2021, 64(11):7483-7506
FEBS J, 2021, 10.1111/febs.15898
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.
Exp Neurol, 2023, 359:114233
Nature, 2022, 10.1038/s41586-022-04967-9
Mol Ther Nucleic Acids, 2022, 27:147-164
S7566 IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.
Nat Commun, 2024, 15(1):668
Cell Stem Cell, 2023, 30(9):1235-1245.e6
Cell Rep, 2022, 38(9):110457
S7954 CP21R7 CP21R7 is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
Cell, 2022, 185(14):2523-2541.e30
Sci Rep, 2022, 12(1):7
ACS Nano, 2021, 10.1021/acsnano.1c06452
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.
Int J Mol Sci, 2023, 24(17)13593
PLoS One, 2023, 18(4):e0284332
J Cell Mol Med, 2022, 26(14):3965-3976
S7253 AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
Sci Rep, 2022, 12(1):7
J Biol Chem, 2021, S0021-9258(21)00485-3
Carcinogenesis, 2020, 41(7):993-1004
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.
BMC Complement Med Ther, 2024, 24(1):28
EMBO Mol Med, 2022, 14(12):e15677
Sci Rep, 2022, 12(1):7
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.
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
S7722 Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
Cell Rep, 2023, 42(3):112187
Plant Physiol, 2022, kiac015
Plant Cell, 2021, koab137
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
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.
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.
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.
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.
E0072 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.
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.
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. 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.

GSK-3阻害剤の選択性比較

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