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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-99021T2310252917-06-9CHIR-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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Cited - GNF4877T114472041073-22-5In houseGNF4877 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
SizeQTY - PHA-767491T6206845714-00-3PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
- $30
SizeQTY Cited - KenPaulloneT2247142273-20-9KenPaullone (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
SizeQTY Cited - AZD1080T1741612487-72-6AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
- $36
SizeQTY Cited - Laduviglusib trihydrochlorideT226571782235-14-6Laduviglusib 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
SizeQTY - CHIR-99021 HClT2310L1797989-42-4CHIR-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
SizeQTY Cited - R547T6312741713-40-6In houseR547 (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.
- $40
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- AZD2858T1957486424-20-8AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.
- $32
SizeQTY - MoringinTN458373255-40-0Moringin 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
SizeQTY - MBM-55T119602083622-09-5MBM-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
SizeQTY - Ginsenoside Rg2T287352286-74-5Ginsenoside Rg2 (Chikusetsusaponin I) is one of the major active components of ginseng, act as an NF-κB inhibitor.
- $31
SizeQTY - KY19382T90252226664-93-1KY19382 (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.
- $60
SizeQTY - VX-11eT3166896720-20-0VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
- $50
SizeQTY - CHIR-124T6350405168-58-3CHIR-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
SizeQTY - IndirubinT6169479-41-4Indirubin (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
SizeQTY - DIF-3T60485113411-17-9DIF-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
SizeQTY Cited - Wnt/β-catenin agonist 2T41094943820-93-7Wnt 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
SizeQTY - Cromolyn sodiumT126015826-37-6Cromolyn sodium (FPL-670) is a chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells.
- $48
SizeQTY - MBM-55ST119612083624-07-9In houseMBM-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.
- $117
SizeQTY - SB 216763T3077280744-09-4SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
- $33
SizeQTY Cited - AT7519T6205844442-38-2AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
- $52
SizeQTY Cited - SNS-032T6049345627-80-7SNS-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
SizeQTY Cited - PHA-767491 hydrochlorideT6940942425-68-5PHA-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
SizeQTY - MeBIOT21966667463-95-8MeBIO 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
SizeQTY - GSK 3 Inhibitor IXT1917667463-62-9GSK 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
SizeQTY Cited - TBBT269517374-26-4TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).
- $38
SizeQTY Cited - LY2090314T1755603288-22-8LY2090314, 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
SizeQTY - A-674563T6139552325-73-2A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
- $47
SizeQTY - A-443654T14072552325-16-3A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
- $84
SizeQTY - TDZD-8T6187327036-89-5TDZD-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
SizeQTY - GSK-3β inhibitor 1T11467187325-53-7GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.
- $43
SizeQTY - CCG 203769T10705410074-60-1CCG 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
SizeQTY - 1-AzakenpaulloneT6358676596-65-91-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.
- $43
SizeQTY - BIO-acetoximeT6787667463-85-6BIO-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.
- $38
SizeQTY - GSK3i XIIIT24111404828-08-6GSK3i XIII (GSK3 inhibitor XIII) is a GSK-3 ATP-binding site inhibitor.
- $59
SizeQTY - GSK-3β inhibitor 2T114711702428-31-6GSK-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
SizeQTY - Indirubin-3'-monoximeT5200160807-49-8Indirubin-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).
- $37
SizeQTY - BikininT1965188011-69-0Bikinin (Abrasin), a potent inhibitor of plant GSK-3/Shaggy-like kinase, activates BR signaling downstream of the BR receptor.
- $39
SizeQTY - TWS119T2166601514-19-6TWS119 is a GSK-3β inhibitor; capable of inducing neuronal differentiation
- $43
SizeQTY - CHIR 98024T3074556813-39-9CHIR 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
SizeQTY - GS87T8605919936-70-2GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.
- $80
SizeQTY - Indirubin-3′-oximeT9138667463-82-3Indirubin-3′-oxime is an effective inhibitor of cyclin-dependent protein kinases, and may play an obligate role in neuronal apoptosis in Alzheimer's disease.
- $34
SizeQTY - GSK-3β inhibitor 3T355541448990-73-5GSK-3β inhibitor 3 is a potent, selective, and irreversible covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with an IC50 of 6.6 μM, and can be used to study acute promyelocytic leukemia.
- $84
SizeQTY - RGB-286638 free baseT2378784210-88-4RGB-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
SizeQTY - TideglusibT3067865854-05-3Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
- $42
SizeQTY Cited - CP21R7T3684125314-13-8CP21R7 (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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