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PI3K/Akt/mTOR signaling GSK-3

GSK-3

Glycogen synthase kinase 3 is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues.Glycogen synthase kinase (GSK-3) is a serine/threonine kinase that phosphorylate either threonine or serine, and this phosphorylation permits a variety of biological activities as glycogen metabolism, cell signaling, cellular transport, and others.SK-3 functions by phosphorylating a serine or threonine residue on its target substrate. A positively charged pocket adjacent to the active site binds a "priming" phosphate group attached to a serine or threonine four residues C-terminal of the target phosphorylation site. The active site, at residues 181, 200, 97, and 85, binds the terminal phosphate of ATP and transfers it to the target location on the substrate .
Cat No. product name
T2310 CHIR99021HOT CHIR-99021 (CT99021) is a GSK-3α/β inhibitor (IC50: 10/6.7 nM).
T9178 GSK-3β inhibitor 1 GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy.
T1881 AR-A014418 AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor.
T6205 AT7519 AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
T3385 Gypenoside XVII Gypenoside XVII confers protection against Aβ25-35-induced neurotoxicity through estrogen receptor-dependent activation of PI3K/Akt pathways, activation of Nrf2...
T6358 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.
T6787 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.
T1917 6-BIO BIO is a specific inhibitor of GSK-3.
T1741 AZD1080 AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
T0256 Lithium citrate tribasic tetrahydrate Lithium Citrate, the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and me...
T1755 LY2090314 LY2090314, an effective GSK-3α/β inhibitor (IC50: 1.5 nM/0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in ...
T2166 TWS119 TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation
T3074 CHIR 98024 CHIR 98024 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 Cdc...
T6139 A674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
T2873 Ginsenoside Rg2 Ginsenoside Rg2 is one of the major active components of ginseng, act as an NF-κB inhibitor.
T1957 AZD2858 AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.
T3067 Tideglusib Tideglusib, a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
T6169 Indirubin Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
T6350 CHIR124 CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
T6049 SNS032 SNS-032 is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1/CDK4. It is also sensitive to CDK7/9 (IC50: 62 nM/4 nM), and n...
T6187 TDZD8 TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
T3077 SB216763 SB216763 is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
T6659 SB415286 SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
T2608 CHIR98014 CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
T1965 Bikinin Bikinin, a potent inhibitor of plant GSK-3/Shaggy-like kinase, activates BR signaling downstream of the BR receptor.
T2695 TBB TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
T2247 KenPaullone Kenpaullone, a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through incr...
T0704 Cyanoacetohydrazide Cyanoacetohydrazide is an anti-TB drug.
T3684 CP21R7 CP21R7 is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth...
T6206 PHA767491 PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
T3166 VX-11e VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
T9025 KY19382 KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt/β-catenin signaling throug...
T8605 GS87 GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.
T24111 GSK3i XIII GSK3i XIII is a GSK-3 ATP-binding site inhibitor.
T8908 4-Chloro-2'-bromoacetophenone 4-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).
TN4637 Neogrifolin Neogrifolin is a potential candidate for osteosarcoma, it can induce concentration- and time-dependent suppression of proliferation and induce apoptosis in U2OS ...
TN4583 Moringin Moringin is a modulator of neuroinflammation via the β-catenin-PPARγ axis, it can activate Wnt canonical pathway by inhibiting GSK3β in a mouse model of exper...
TN4424 Lecanoric acid Lecanoric acid shows antioxidant activity with an IC50 value of 79-95 ug/ml, it at 100 ug/ml conc. shows high growth stimulating activity in terms of increased d...
TN4263 Isoangustone A Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation ...
TN4046 Excisanin A ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a pote...
TMA0291 Dehydroglyasperin D Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 h...
TN3319 9-Hydroxycanthin-6-one 9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as ...
TN2995 4,10-Aromadendranediol 4,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the treatm...
TN2775 2-Methoxystypandrone 2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the infla...
T2S0606 Bakkenolide A Bakkenolide A has antifeedant and growth inhibitory effects on neonate variegated cutworms, it inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related sign...
T17019 TCS 21311 TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectivel...
T1778 AT 7519 hydrochloride salt AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.
T10786 Charantin Charantin is a steroidal saponin isolated from Momordica charantia. It increases the release of insulin and slowing down gluconeogenesis. Charantin can inhibit G...
T11471 GSK-3β inhibitor 2 GSK-3β inhibitor 2 is a selective and orally active GSK-3β inhibitor (IC50: 1.1 nM). GSK-3β inhibitor 2 can cross the blood-brain barrier with the potential f...
T11468 GSK-3 inhibitor 1 GSK-3 inhibitor 1 is a GSK-3 inhibitor.
T11467 GSK-3β inhibitor 1 GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.
T10606 BRD0705 BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) ...
T14613 BIP-135 BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor. With IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuropro...
T14066 9-ING-41 9-ING-41 is a glycogen synthase kinase-3 inhibitor.
T10202 A 1070722 A 1070722 is a potent and selective GSK-3 inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. It can penetrate the blood-brain barrier (BBB) and accumul...
TN1819 Kaempferol 3-neohesperidoside Kaempferol 3-neohesperidoside is a flavonoid. Kaempferol 3-neohesperidoside exhibits insulinomimetic effect on the rat soleus muscle.
T7473 5-Bromoindole 5-bromoindole is a potential inhibitor of glycogen synthase kinase 3 (GSK-3)and an important pharmaceutical chemical intermediate
T5956 VP3.15 dihydrobromide VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE7- glycogen synthase kinase (GSK)3 inhibitor(with IC50s of 1....
T5200 Indirubin-3'-monoxime Indirubin-3'-oxime is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E).
T6940 PHA767491 HCl PHA-767491 is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity...
T2261 IM12 IM-12, an effective GSK-3β inhibitor(IC50=53 nM), regulates Wnt signalling.
CHIR99021 HOT
T2310CAS 252917-06-9
CHIR-99021 (CT99021) is a GSK-3α/β inhibitor (IC50: 10/6.7 nM).
GSK-3β inhibitor 1
T9178CAS 3367-88-2
GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy.
AR-A014418
T1881CAS 487021-52-3
AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor.
AT7519
T6205CAS 844442-38-2
AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
Gypenoside XVII
T3385CAS 80321-69-3
Gypenoside XVII confers protection against Aβ25-35-induced neurotoxicity through estrogen receptor-dependent activation of PI3K/Akt pathways, activation of Nrf2...
1-Azakenpaullone
T6358CAS 676596-65-9
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.
BIO-acetoxime
T6787CAS 667463-85-6
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.
6-BIO
T1917CAS 667463-62-9
BIO is a specific inhibitor of GSK-3.
AZD1080
T1741CAS 612487-72-6
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
Lithium citrate tribasic tetrahydrate
T0256CAS 6080-58-6
Lithium Citrate, the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and me...
LY2090314
T1755CAS 603288-22-8
LY2090314, an effective GSK-3α/β inhibitor (IC50: 1.5 nM/0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in ...
TWS119
T2166CAS 601514-19-6
TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation
CHIR 98024
T3074CAS 556813-39-9
CHIR 98024 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 Cdc...
A674563
T6139CAS 552325-73-2
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
Ginsenoside Rg2
T2873CAS 52286-74-5
Ginsenoside Rg2 is one of the major active components of ginseng, act as an NF-κB inhibitor.
AZD2858
T1957CAS 486424-20-8
AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.
Tideglusib
T3067CAS 865854-05-3
Tideglusib, a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
Indirubin
T6169CAS 479-41-4
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
CHIR124
T6350CAS 405168-58-3
CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
SNS032
T6049CAS 345627-80-7
SNS-032 is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1/CDK4. It is also sensitive to CDK7/9 (IC50: 62 nM/4 nM), and n...
TDZD8
T6187CAS 327036-89-5
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
SB216763
T3077CAS 280744-09-4
SB216763 is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
SB415286
T6659CAS 264218-23-7
SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β.
CHIR98014
T2608CAS 252935-94-7
CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Bikinin
T1965CAS 188011-69-0
Bikinin, a potent inhibitor of plant GSK-3/Shaggy-like kinase, activates BR signaling downstream of the BR receptor.
TBB
T2695CAS 17374-26-4
TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
KenPaullone
T2247CAS 142273-20-9
Kenpaullone, a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through incr...
Cyanoacetohydrazide
T0704CAS 140-87-4
Cyanoacetohydrazide is an anti-TB drug.
CP21R7
T3684CAS 125314-13-8
CP21R7 is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth...
PHA767491
T6206CAS 845714-00-3
PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
VX-11e
T3166CAS 896720-20-0
VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
KY19382
T9025CAS 2226664-93-1
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt/β-catenin signaling throug...
GS87
T8605CAS 919936-70-2
GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.
GSK3i XIII
T24111CAS 404828-08-6
GSK3i XIII is a GSK-3 ATP-binding site inhibitor.
4-Chloro-2'-bromoacetophenone
T8908CAS 536-38-9
4-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).
Neogrifolin
TN4637CAS 23665-96-5
Neogrifolin is a potential candidate for osteosarcoma, it can induce concentration- and time-dependent suppression of proliferation and induce apoptosis in U2OS ...
Moringin
TN4583CAS 73255-40-0
Moringin is a modulator of neuroinflammation via the β-catenin-PPARγ axis, it can activate Wnt canonical pathway by inhibiting GSK3β in a mouse model of exper...
Lecanoric acid
TN4424CAS 480-56-8
Lecanoric acid shows antioxidant activity with an IC50 value of 79-95 ug/ml, it at 100 ug/ml conc. shows high growth stimulating activity in terms of increased d...
Isoangustone A
TN4263CAS 129280-34-8
Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation ...
Excisanin A
TN4046CAS 78536-37-5
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a pote...
Dehydroglyasperin D
TMA0291CAS 517885-72-2
Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 h...
9-Hydroxycanthin-6-one
TN3319CAS 138544-91-9
9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as ...
4,10-Aromadendranediol
TN2995CAS 70051-38-6
4,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the treatm...
2-Methoxystypandrone
TN2775CAS 85122-21-0
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the infla...
Bakkenolide A
T2S0606CAS 19906-72-0
Bakkenolide A has antifeedant and growth inhibitory effects on neonate variegated cutworms, it inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related sign...
TCS 21311
T17019CAS 1260181-14-3
TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectivel...
AT 7519 hydrochloride salt
T1778CAS 902135-91-5
AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.
Charantin
T10786CAS 57126-62-2
Charantin is a steroidal saponin isolated from Momordica charantia. It increases the release of insulin and slowing down gluconeogenesis. Charantin can inhibit G...
GSK-3β inhibitor 2
T11471CAS 1702428-31-6
GSK-3β inhibitor 2 is a selective and orally active GSK-3β inhibitor (IC50: 1.1 nM). GSK-3β inhibitor 2 can cross the blood-brain barrier with the potential f...
GSK-3 inhibitor 1
T11468CAS 603272-51-1
GSK-3 inhibitor 1 is a GSK-3 inhibitor.
GSK-3β inhibitor 1
T11467CAS 187325-53-7
GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.
BRD0705
T10606CAS 2056261-41-5
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) ...
BIP-135
T14613CAS 941575-71-9
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor. With IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuropro...
9-ING-41
T14066CAS 1034895-42-5
9-ING-41 is a glycogen synthase kinase-3 inhibitor.
A 1070722
T10202CAS 1384424-80-9
A 1070722 is a potent and selective GSK-3 inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. It can penetrate the blood-brain barrier (BBB) and accumul...
Kaempferol 3-neohesperidoside
TN1819CAS 32602-81-6
Kaempferol 3-neohesperidoside is a flavonoid. Kaempferol 3-neohesperidoside exhibits insulinomimetic effect on the rat soleus muscle.
5-Bromoindole
T7473CAS 10075-50-0
5-bromoindole is a potential inhibitor of glycogen synthase kinase 3 (GSK-3)and an important pharmaceutical chemical intermediate
VP3.15 dihydrobromide
T5956CAS 1281681-33-1
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE7- glycogen synthase kinase (GSK)3 inhibitor(with IC50s of 1....
Indirubin-3'-monoxime
T5200CAS 160807-49-8
Indirubin-3'-oxime is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E).
PHA767491 HCl
T6940CAS 942425-68-5
PHA-767491 is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity...
IM12
T2261CAS 1129669-05-1
IM-12, an effective GSK-3β inhibitor(IC50=53 nM), regulates Wnt signalling.