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PI3K/Akt/mTOR signaling
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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
SizeQTY
Cited - GSK-3 Inhibitor XIIIT78578404828-14-4In houseGSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.
- $169
SizeQTY
- GSK3a-IN-38T776711062138-03-7GSK3a-IN-38 is a novel small molecule compound that has inhibitory effects on GSK-3a.
- $195
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 - GS87T8605919936-70-2GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.
- $133
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.
- $195
SizeQTY - GSK-3 inhibitor 3T773422227279-84-5In houseGSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.
- $195
SizeQTY - GSK-3 Inhibitor 5T7755420099-89-2GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).
- $29
SizeQTY - 4-Chloro-2'-bromoacetophenoneT8908536-38-94-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).
- $50
SizeQTY - GSK3-IN-2T73270380450-97-5GSK3-IN-2 is a potent GSK3 inhibitor for the treatment of diabetes and neurodegenerative diseases.
- $72
SizeQTY - GSK-3 inhibitor 4T773412227279-83-4In houseGSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.
- $350
SizeQTY - Aloisine BT69188496864-14-3In houseAloisine B (AloisineB) inhibited cyclin-dependent kinase and glycogen synthase kinase with IC50 values of 0.85 µM and 0.75 µM, respectively. Aloisine B has antiviral activity and can be used to study Alzheimer's, diabetes, HIV and Parkinson's.
- $350
SizeQTY - GSK-3β inhibitor 12T60472784170-07-6GSK-3β inhibitor 12 is a selective GSK-3β inhibitor.GSK-3β inhibitor 12 inhibits 49.11% of 25 μM GSK-3β activity and 37.11% of 50 μM GSK-3β activity.GSK-3β inhibitor 12 can be used for the study of Parkinson's in the presence of lipopolysaccharide induction.
- $83
SizeQTY - Ceftriaxone SodiumT66175958633-51-7Ceftriaxone Sodium is a broad-spectrum β-lactam tertiary cephalosporin antibiotic with anti-inflammatory, antitumor, antibacterial, and antioxidant activities.Ceftriaxone Sodium is a covalent GSK3β and Aurora B inhibitor used in the study of sepsis and infective endocarditis.
- $39
SizeQTY Cited - 3F8T22180159109-11-2In house3F8 is a selective GSK-3β inhibitor that can be used as a new tool and potential therapeutic candidate compound for GSK3-related diseases, and can be used in the study of neurological disorders and cancer.
- $115
SizeQTY - CDK8-IN-12T720482613307-67-6In houseCDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.
- $79
SizeQTY - GSK3-IN-4T64366748145-19-9GSK3-IN-4 is a GSK-3 inhibitor with IC50 of 0.101-1 μM of GSK-3α and GSK-3β in Calipe Assay.
- $117
SizeQTY - GSK-3 inhibitor 1T11468603272-51-1In houseGSK-3 inhibitor 1 is a GSK-3 inhibitor.
- $106
SizeQTY - $106
- GSK-3β inhibitor 8T355561139875-74-3In houseGSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.
- $110
SizeQTY - ARN25068T613602649882-80-2In houseARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].
- $115
SizeQTY - 5-Iodo-indirubin-3'-monoximeT10172331467-03-9In house5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20 and 25 nM).
- $297
SizeQTY - EHT 1610T152041425945-60-3In houseEHT 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.
- $147
SizeQTY - 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.
- $45
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 - TideglusibT3067865854-05-3Tideglusib (NP031112), a non-ATP competitive inhibitor of glycogen synthase kinase 3 (GSK-3), is with anti-inflammatory and neuroprotective activities.
- $39
SizeQTY Cited - AR-A014418T1881487021-52-3AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
- $45
SizeQTY Cited - AZD1080T1741612487-72-6AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor.
- $36
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 - SNS-032T6049345627-80-7SNS-032 (BMS-387032) 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 no effect on CDK6.
- $43
SizeQTY Cited - SB 216763T3077280744-09-4SB 216763 (SB216763) is an effective and specific GSK-3α/β inhibitor (IC50: 34.3 nM).
- $33
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 - 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 - 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 - Excisanin ATN404678536-37-5ExcisaninA 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 potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).
- $980
SizeQTY - GSK-3β inhibitor 14T67856863004-48-2GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.
- $147
SizeQTY - Isoangustone ATN4263129280-34-8Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
- $540
SizeQTY - GSK3-IN-1T9987478482-74-5GSK3-IN-1 is a GSK3B-glycogen synthase kinase-3 beta inhibitor.
- $44
SizeQTY - 5-BromoindoleT747310075-50-05-bromoindole is a potential inhibitor of glycogen synthase kinase 3 (GSK-3)and an important pharmaceutical chemical intermediate
- $39
SizeQTY - 2-MethoxystypandroneTN277585122-21-02-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant
- $520
SizeQTY - GSK3β inhibitor IIT21956478482-75-6GSK3β inhibitor II is a GSK3β inhibitor. GSK3β inhibitor II exhibits the research potential of Alzheimer's disease (AD).
- $43
SizeQTY - NeogrifolinTN463723665-96-5Neogrifolin is a potential candidate for osteosarcoma, it can induce concentration- and time-dependent suppression of proliferation and induce apoptosis in U2OS and MG63 osteosarcoma cell lines; it exhibits inhibitory activity against nitric oxide (NO) production stimulated by lipopolysaccharide (LPS) in RAW 264.7 cells with the IC50value of 23.3 microM. Neogrifolin possesses antimicrobial activities against Bacillus cereus and Enterococcus faecalis, the MIC values of 20 and 0.5 microg/mL, respectively.
- $1,790
SizeQTY - hAChE-IN-5T82243hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting inhibitory potency with IC50 values of 0.17 μM for both enzymes. Additionally, it demonstrates potent glycogen synthase kinase 3 beta (GSK3β) inhibition with an IC50 of 0.21 μM. The compound is an effective inhibitor of tau protein and Aβ1-42 peptide self-aggregation. It can virtually bind the peripheral anionic site (PAS), preventing amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) underpins its utility in the development of multitargeted anti-Alzheimer’s agents [1].
- Inquiry Price
SizeQTY - 9-Hydroxycanthin-6-oneTN3319138544-91-99-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 well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α.
- $2,298
SizeQTY - CharantinT1078657126-62-2Charantin is a steroidal saponin isolated from Momordica charantia. It increases the release of insulin and slowing down gluconeogenesis. Charantin can inhibit GSK-3.
- Inquiry Price
SizeQTY - 4,10-AromadendranediolTN299570051-38-64,10-Aromadendranediol exhibits neurite outgrowth-inducing activity in neurons via activation of the ERK signaling pathway, which may be beneficial to the treatment of brain diseases.
- $620
SizeQTY - PF-04802367T96111962178-27-3PF-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.
- $74
SizeQTY - C-Peptide 1 (rat)T8012441475-27-8C-Peptide 1 (rat), a β-catenin/GSK-3β activator and regulator of the Wnt/β-catenin signaling pathway, is utilized in cancer research [1].
- Inquiry Price
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 - BRD0209T268941597439-87-6BRD0209 is a highly selective and potent GSK3 inhibitor.
- $58
SizeQTY - Dehydroglyasperin DTMA0291517885-72-2Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 human colorectal cancer cells through direct interaction with phosphatidylinositol 3-kinase; it also mediates suppression of both COX-2 expression and the MLK3 signalling pathway through direct binding and inhibition of MLK3. Dehydroglyasperin D shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
- $1,670
SizeQTY
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