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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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Laduviglusib 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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Tideglusib Cited
T3067865854-05-3
Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
- $39
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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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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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GSK-3 inhibitor 4
T773412227279-83-4In house
GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.
- $350
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TBB 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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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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CitedA-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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Ginsenoside Rg2 Cited
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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CitedWnt/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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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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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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CitedKenPaullone 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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CitedSB 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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CitedKY19382
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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Moringin
TN458373255-40-0
Moringin is an isothiocyanate obtained from myrosinase-mediated hydrolysis of the glucosinolate precursor glucoMoringin present in Moringa oleifera seeds. Moringin has anti-inflammatory and antioxidative properties.
- $138
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Indirubin
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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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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CitedCHIR-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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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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IM-12
T22611129669-05-1
IM-12, an effective GSK-3β inhibitor(IC50=53 nM), regulates Wnt signalling.
- $48
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CP21R7
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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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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BRD0705
T106062056261-41-5
BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM).
- $91
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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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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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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-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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R547
T6312741713-40-6In house
R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.
- $45
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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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TWS119
T2166601514-19-6
TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation
- $43
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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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RGB-286638 free base
T2378784210-88-4
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
- $39
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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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BIO-acetoxime
T6787667463-85-6
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.
- $30
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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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BIP-135
T14613941575-71-9
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50 values of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively, and exhibits neuroprotective effects [1].
- $29
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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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PF-04802367
T96111962178-27-3
PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. It shows desirable central nervous system (CNS) properties and potency. It is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.
- $44
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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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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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