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PI3K/Akt/mTOR signaling Filter
PI3K/Akt/mTOR signalingGSK-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. First discovered in 1980 as a regulatory kinase for its namesake, Glycogen synthase, GSK-3 has since been identified as a kinase for over 100 different proteins in a variety of different pathways. In mammals GSK-3 is encoded by two paralogous genes, GSK-3 alpha (GSK3A) and GSK-3 beta (GSK3B). GSK-3 has recently been the subject of much research because it has been implicated in a number of diseases, including Type II diabetes (diabetes mellitus type 2), Alzheimer's disease, inflammation, cancer, and bipolar disorder.
CHIR-99021
Cited
T2310252917-06-9
CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
- $36
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CitedGNF4877
T114472041073-22-5In house
GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.
- $127
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PHA-767491 Cited
T6206845714-00-3
PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
- $30
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CitedLaduviglusib trihydrochloride
T226571782235-14-6
Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt β-catenin signaling. Laduviglusib trihydrochloride induces autophagy.
- $36
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KenPaullone Cited
T2247142273-20-9
KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.
- $32
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CitedMBM-55
T119602083622-09-5
MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
- $187
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AZD2858
T1957486424-20-8
AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.
- $32
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CHIR-99021 HCl Cited
T2310L1797989-42-4
CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].
- $30
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CitedEHT 1610
T152041425945-60-3In house
EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.
- $88
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AZD1080 Cited
T1741612487-72-6
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
- $36
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CitedLY2090314
T1755603288-22-8
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 trials studying the treatment of Leukemia, Advanced Cancer, and Pancreatic Cancer.
- $41
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Ginsenoside Rg2
T287352286-74-5
Ginsenoside Rg2 (Chikusetsusaponin I) is one of the major active components of ginseng, act as an NF-κB inhibitor.
- $31
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KY19382
T90252226664-93-1
KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-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 through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
- $100
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A-443654
T14072552325-16-3
A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
- $84
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DIF-3 Cited
T60485113411-17-9
DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
- $93
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CitedTBB Cited
T269517374-26-4
TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).
- $38
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CitedIndirubin
T6169479-41-4
Indirubin (Couroupitine B) is a potent inhibitor of cyclin-dependent kinases and GSK-3β, with IC50 values of approximately 5 µM and 0.6 µM, respectively.
- $45
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Wnt/β-catenin agonist 2
T41094943820-93-7
Wnt β-catenin agonist 2 activates Wnt β-catenin signaling and is an effective Wnt agonist. Wnt β-catenin agonist 2 can be used in the study of diseases related to signal transduction and is closely related to cancer invasion and metastasis.
- $49
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CHIR-124
T6350405168-58-3
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.
- $35
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VX-11e
T3166896720-20-0
VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
- $50
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Cromolyn sodium
T126015826-37-6
Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.
- $48
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Bikinin
T1965188011-69-0
Bikinin (Abrasin), a potent inhibitor of plant GSK-3 Shaggy-like kinase, activates BR signaling downstream of the BR receptor.
- $39
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Kaempferol 3-neohesperidoside
TN181932602-81-6
Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside), a flavonoid compound, exhibits an insulinomimetic effect on the rat soleus muscle.
- $56
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AT7519 Cited
T6205844442-38-2
AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
- $52
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CitedMBM-55S
T119612083624-07-9In house
MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
- $195
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SB 216763 Cited
T3077280744-09-4
SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
- $33
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CitedSNS-032 Cited
T6049345627-80-7
SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.
- $43
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CitedCP21R7
T3684125314-13-8
CP21R7 (CP21) 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 muscle and endothelial cells. CP21R7 can be combined with BMP4 to commit human pluripotent stem cells to a mesodermal fate.
- $57
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GSK 3 Inhibitor IX Cited
T1917667463-62-9
GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α β and CDK1-cyclinB complex. It inhibits (GSK-3α β) CDK1 CDK5 activity with IC50 values of 5 nM 320 nM 83 nM, respectively.
- $37
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CitedMeBIO
T21966667463-95-8
MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1/CyclinB, respectively. MeBIO does not affect GSK-3β.
- $33
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K 00546
T21950443798-47-8
K 00546 is a potent inhibitor of cellular cyclin kinases (CDK1 and CDK2) and CDC2-like kinases (CLK1 and CLK3) used in the study of cancer and immune-related diseases.
- $98
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PHA-767491 hydrochloride
T6940942425-68-5
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 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 against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.
- $43
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Indirubin-3'-monoxime
T5200160807-49-8
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).
- $30
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GSK-3 inhibitor 1
T11468603272-51-1In house
GSK-3 inhibitor 1 is a GSK-3 inhibitor.
- $106
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A-674563
T6139552325-73-2
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
- $47
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GSK-3β inhibitor 1
T11467187325-53-7
GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.
- $71
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CCG 203769
T10705410074-60-1
CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
- $81
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1-Azakenpaullone
T6358676596-65-9
1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1 cyclin B and CDK5 p25.
- $72
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Indirubin-3′-oxime
T9138667463-82-3
Indirubin-3′-oxime is an effective inhibitor of cyclin-dependent protein kinases, and may play an obligate role in neuronal apoptosis in Alzheimer's disease.
- $39
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TDZD-8
T6187327036-89-5
TDZD-8 (NP 01139) is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
- $42
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ALSTERPAULLONE
T7426237430-03-4
Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec
- $53
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GSK3i XIII
T24111404828-08-6
GSK3i XIII (GSK3 inhibitor XIII) is a GSK-3 ATP-binding site inhibitor.
- $101
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GSK-3β inhibitor 2
T114711702428-31-6
GSK-3β inhibitor 2 (5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-) is a BBB-crossing and selective inhibitor of GSK-3β (IC50 = 1.1 nM). GSK-3β inhibitor 2 can be used in studies about Alzheimer's disease.
- $50
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CHIR-98014
T2608252935-94-7
CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
- $68
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BRD5648
T106082056261-42-6
BRD5648 ((R)-BRD0705) is an inactive (R)-enantiomer of BRD0705, a GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM, used in acute myeloid leukemia [AML] studies.
- $63
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TWS119
T2166601514-19-6
TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation
- $43
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CHIR 98024
T3074556813-39-9
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 Cdc2 and ERK2.
- $37
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