Catalog No.
Product Name
Application
Product Information
Citations
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YAP-TEAD Inhibitor
TED-347 is a potent irreversible allosteric inhibitor of the YAP-TEAD protein-protein interaction, exhibiting an EC50 of 5.9 μM for the TEAD4-Yap1 complex. The compound covalently binds to Cys-367 within the central pocket of TEAD4, with a Ki value of 10.3 μM. By inhibiting TEAD transcriptional activity, TED-347 demonstrates significant antitumor potential, making it a valuable tool for cancer research and therapeutic studies focused on the Hippo signaling pathway. -
YAP-TEAD Activator
TT-10 is a potent activator of the YES-associated protein (YAP) and transcriptional enhancer factor domain (TEAD) signaling pathway. This compound enhances YAP-TEAD activity, which is crucial in regulating cell proliferation and survival. TT-10 is particularly useful for investigating heart diseases associated with cardiomyocyte loss, providing potential insights into therapeutic strategies for cardiac regeneration. -
YAP/TAZ-TEAD Inhibitor
SWTX-143 is an orally active inhibitor of the YAP/TAZ-TEAD signaling pathway, targeting the palmitoylation pocket across all four TEAD isoforms. This compound demonstrates irreversible and selective suppression of YAP/TAZ-TEAD transcriptional activity, highlighting its potential in antitumor research. SWTX-143 serves as a valuable tool for investigating the mechanistic roles of YAP/TAZ-TEAD in oncogenesis and therapeutic strategies against cancer. -
YAP Antagonist
Super-TDU is a selective YAP antagonist that disrupts the YAP-TEAD interaction. This compound has demonstrated the ability to inhibit tumor growth in gastric cancer mouse models, making it a valuable tool for research in cancer biology and therapeutic development targeting the hippo signaling pathway. Its application in studying YAP-related signaling pathways offers insights into potential treatments for various malignancies. -
TEAD-YAP/TAZ Inhibitor
YAP/TAZ Inhibitor-2 is a potent and orally bioactive compound that targets the TEAD-YAP/TAZ signaling pathway, demonstrating an EC50 of 3 nM. This inhibitor exhibits significant anti-proliferative effects, making it a valuable tool for research into tumorigenesis and cancer biology. Its antitumor activity further supports its application in studies focused on cellular proliferation and tumor growth regulation. -
YAP/TAZ-TEAD Inhibitor
MSC-4106 is a potent, orally active inhibitor targeting the YAP/TAZ-TEAD signaling pathway. This compound effectively inhibits the auto-palmitoylation of TEAD1 and TEAD3, demonstrating significant biological activity. MSC-4106 has been shown to exert inhibitory effects in the NCI-H226 tumor xenograft model, making it a valuable tool for cancer research and therapeutic development. -
YAP-TEAD PPI Inhibitor
YAP-TEAD-IN-2 is a potent inhibitor of the YAP-TEAD protein-protein interaction, exhibiting an IC50 value of 2.7 nM. This compound selectively interferes with the binding affinity between YAP and TEAD, thereby modulating the Hippo signaling pathway. YAP-TEAD-IN-2 is useful in various research applications, particularly in studies of cancer biology and cellular growth regulation, where the dysregulation of this interaction is implicated. -
YAP-TEAD Inhibitor
YTP-17 is a potent inhibitor of the YAP-TEAD protein-protein interaction, exhibiting an IC50 of 4 nM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. YTP-17 can be utilized to investigate the role of the YAP-TEAD pathway in various tumorigenic processes. -
YAP-TEAD Interation Inhibitor
VS3 is a selective inhibitor of the YAP-TEAD interaction, effectively disrupting their binding by targeting TEAD4 Interface 3 with a dissociation constant (Kd) of 6 μM. This compound demonstrates significant anti-proliferative effects in various cancer cell lines, including HT29, HCT116, and A2780. VS3 is a valuable tool for investigating signaling pathways in colorectal adenocarcinoma and ovarian cancer research. -
YAP/TAZ-TEAD Inhibitor
YAP/TAZ-TEAD-IN-3 is a potent inhibitor of the YAP/TAZ-TEAD protein-protein interaction, exhibiting an IC50 of 1.8 nM. This compound serves as a valuable tool for studies involving the Hippo signaling pathway and can be utilized in the development of PROTACs targeting TEAD1, such as PROTAC TEAD degrader-2. Its application extends to cellular and molecular research focused on cancer biology and tissue development regulation. -
YAP1 Inhibitor
Hapalindole Q is a selective YAP1 inhibitor that functions by inducing the degradation of the Hippo pathway transcription factor YAP1 through the chaperone-mediated autophagy (CMA) pathway. With a dissociation constant (Kd) of 9.13 μM, Hapalindole Q effectively hinders Rab7-mediated autophagosome and lysosome fusion, resulting in a decrease in overall autophagy levels while preserving lysosomal function. This compound is relevant for cancer research, particularly in the context of liver and breast cancer investigations. -
CDK2/GSK3β Inhibitor
Tagtociclib hydrate is a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2) and glycogen synthase kinase 3 beta (GSK3β), displaying inhibition constants of 1.16 nM and 537.81 nM, respectively. This compound demonstrates significant anti-tumor activity, particularly in cancers characterized by cyclin E1 amplification. Tagtociclib hydrate serves as a valuable research tool for studying cell cycle regulation and therapeutic strategies targeting kinase pathways in cancer biology. -
GSK-3β Inhibitor
GSK-3β Inhibitor 2 is a selective and potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 1.1 nM. This compound is orally active and is capable of penetrating the blood-brain barrier, making it a valuable tool for neurological research. GSK-3β Inhibitor 2 holds potential for therapeutic applications in Alzheimer's disease and other neurodegenerative conditions by modulating signaling pathways associated with neuronal survival and function. -
β-catenin/GSK-3β Activator
C-Peptide 1 (rat) is a peptide that functions as an activator of β-catenin and GSK-3β. Its primary mechanism involves the regulation of the Wnt/β-catenin signaling pathway, which plays a crucial role in cellular processes such as proliferation and differentiation. C-Peptide 1 (rat) is utilized in cancer research, contributing to studies aimed at understanding tumorigenesis and potential therapeutic interventions. -
PROTAC GSK-3β Degrader
PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions. -
GSK-3 Inhibitor
PF-04802367 is a highly selective glycogen synthase kinase 3 (GSK-3) inhibitor, demonstrating an IC50 of 2.1 nM in recombinant human GSK-3β assays and 1.1 nM in ADP-Glo assays. This compound effectively inhibits both GSK-3 isoforms, GSK-3α and GSK-3β, with IC50 values of 10.0 nM and 9.0 nM, respectively, as measured by mobility shift assays. PF-04802367 is distinguished by its favorable central nervous system (CNS) properties, making it a valuable tool in neurobiological research and related therapeutic investigations. -
GSK3α/GSK3β PROTAC Degrader
PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions. -
GSK3β/AβOs Inhibitor
Cu(II)GTSM is a cell-permeable copper complex that acts as a potent inhibitor of glycogen synthase kinase 3 beta (GSK3β). This compound significantly reduces the formation of amyloid-beta oligomers (AβOs) and lowers tau phosphorylation levels, thereby influencing key pathways related to neurodegenerative diseases. Additionally, Cu(II)GTSM diminishes the abundance of amyloid-beta trimers and exhibits potential as an anticancer and antimicrobial agent, making it valuable for various research applications in disease modeling and therapeutic development. -
GSK3β Inhibitor
BRD3731 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), demonstrating an IC50 of 15 nM for GSK3β and 215 nM for GSK3α. This compound exhibits significant potential in research related to post-traumatic stress disorder (PTSD), various psychiatric disorders, diabetes, and neurodegenerative diseases. Its specificity and potency make it a valuable tool for studying GSK3β-related signaling pathways and therapeutic interventions. -
CDKL5/GSK3 Inhibitor
SGC-CDKL5/GSK3 is a selective inhibitor targeting CDKL5 and GSK3α/β. This compound demonstrates potent inhibition, with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α, as assessed by the NanoBRET assay. Its specificity and efficacy make it a valuable tool for investigating central nervous system diseases and related biological pathways. -
GSK-3β Inhibitor
GSK-3β inhibitor 22 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 3.1 nM. This compound is suitable for research applications focused on neurodegenerative diseases, particularly Alzheimer's disease. It provides a valuable tool for investigating the role of GSK-3β in cellular pathways and potential therapeutic interventions in related pathologies. -
GSK3α/β Inhibitor
BRD0209 is a potent and selective dual inhibitor of glycogen synthase kinase 3 alpha and beta (GSK3α/β), exhibiting IC50 values of 19 nM and 5 nM, respectively. This reversible ATP-competitive inhibitor demonstrates fast-off kinetics with a Ki of 4.2 nM. As a tricyclic pyrazolotetrahydroquinolinone compound, BRD0209 is primarily utilized in the investigation of mood disorders and related neurobiological research. -
GSK-3 Inhibitor
GSK-3 Inhibitor 3 is a selective inhibitor targeting glycogen synthase kinase 3 (GSK-3) with notable brain penetration. It exhibits low nanomolar potency, with IC50 values of 0.35 nM for GSK-3α and 0.25 nM for GSK-3β. This compound effectively reduces tau protein phosphorylation at the S396 site in a triple-transgenic mouse model of Alzheimer's disease, demonstrating an IC50 of 10 nM. GSK-3 Inhibitor 3 is valuable for research into neurological diseases and related signaling pathways. -
GSK3 Inhibitor
CHIR 98024 is a potent glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM. This compound modulates various signaling pathways, contributing to cellular processes such as proliferation, differentiation, and metabolism. CHIR 98024 is utilized in research exploring its therapeutic potential in neurodegenerative diseases, cancer, and other disorders associated with GSK3 dysregulation. -
GSK3β Inhibitor
GSK-3β Inhibitor XI is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with a potent Ki value of 25 nM. This compound enhances glycogen synthase (GS) activity, making it valuable for investigations into metabolic disorders such as type 2 diabetes and neurodegenerative diseases, including Alzheimer’s disease. Its specificity and potency render it a useful tool for elucidating the role of GSK-3β in various biological processes and therapeutic contexts. -
GSK-3
GSK3-IN-7 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3). This small molecule exhibits potent GSK-3 inhibition, which is critical for modulating cellular signaling pathways involved in glucose metabolism and neurodegenerative diseases. GSK3-IN-7 is utilized in research applications focused on the development of therapeutic strategies for conditions such as diabetes, Alzheimer's disease, and cancer. -
GSK3 Inhibitor
SAR502250 is a potent and selective ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3) with an IC50 of 12 nM for human GSK-3β. This compound is orally active and exhibits the ability to penetrate the blood-brain barrier. SAR502250 demonstrates antidepressant-like activity and is applicable for research into Alzheimer's disease and related neurological conditions. -
GSK3/CDK9 Inhibitor
ABC1183 is a selective dual inhibitor targeting GSK3 and CDK9, effectively inhibiting GSK3β, GSK3α, and CDK9/cyclin T1 with IC50 values of 657 nM, 327 nM, and 321 nM, respectively. This compound exhibits notable anti-inflammatory and anti-tumor activities, making it a valuable tool for cancer research and inflammation-related studies. Its ability to modulate critical signaling pathways positions ABC1183 as a promising candidate for further investigation in therapeutic applications. -
GSK-3 Inhibitor
GSK3-IN-1 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3) with an IC50 value of 12 μM. This compound is involved in various signaling pathways and plays a critical role in glucose metabolism and insulin signaling. GSK3-IN-1 is particularly relevant for research applications focused on diabetes and other metabolic disorders. -
GSK3β Inhibitor
GSK3β Inhibitor II is a selective inhibitor targeting glycogen synthase kinase 3 beta (GSK3β). This compound exhibits significant activity in modulating GSK3β activity, making it a valuable tool for studying signaling pathways implicated in neurodegenerative diseases such as Alzheimer’s disease. Its use facilitates research aimed at elucidating the roles of GSK3β in cellular processes and potential therapeutic strategies for AD. -
GSK-3/CDK5/CDK2 Inhibitor
GSK-3/CDK5/CDK2-IN-1 is a potent inhibitor targeting GSK-3, CDK5, and CDK2. This imidazole derivative has demonstrated effectiveness in modulating pathways relevant to tumorigenesis and neurodegenerative disorders. Its ability to inhibit these kinases makes it a valuable tool for investigating mechanisms underlying cancer proliferation and neurodegeneration. -
GSK-3β Inhibitor
(E/Z)-GSK-3β inhibitor 1 is a racemic mixture comprising both (E)- and (Z)-isomers targeting glycogen synthase kinase 3β (GSK-3β). This compound exhibits significant antidiabetic activity, with an IC50 value of 4.9 nM, making it a valuable tool for studying pathways related to glucose metabolism and insulin signaling. Its inhibition of GSK-3β provides insights into potential therapeutic strategies for diabetes and related metabolic disorders. -
GSK-3 Inhibitor
L803-mts is a selective, substrate-competitive inhibitor of glycogen synthase kinase 3 (GSK-3) with an IC50 of 40 μM. This compound has been shown to significantly reduce amyloid-beta (Aβ) deposits and improve cognitive deficits in the 5XFAD mouse model of Alzheimer's disease. Additionally, L803-mts exhibits antidepressant-like effects, as demonstrated in the forced swimming test, making it a valuable tool for studying neurodegenerative and mood disorders. -
GSK-3β Inhibitor
GSK-3β inhibitor 8 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 64 nM. This thiophenacil derivative targets the Wnt signaling pathway, leading to its negative regulation and promoting β-cell proliferation. GSK-3β inhibitor 8 is valuable for research involving cell signaling, diabetes, and regenerative medicine applications. -
GSK-3β Inhibitor
COB-187 is a selective and potent ATP-competitive inhibitor of Glycogen Synthase Kinase 3 beta (GSK-3β). This compound operates through a reversible mechanism dependent on Cysteine (Cys)-199, effectively inhibiting GSK-3β activity. COB-187 is shown to reduce cytokine production induced by lipopolysaccharides (LPS) and decreases CXCL10 production triggered by SARS-CoV-2 spike protein, making it relevant for research in inflammation and viral response studies. -
GSK-3 Inhibitor
GSK-3 Inhibitor XIII is a potent ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3), exhibiting a Ki value of 24 nM. It effectively modulates GSK-3 activity, making it a valuable tool for studying various biological processes, including cell growth, differentiation, and metabolism. This inhibitor is particularly relevant for research in cancer, neurodegenerative diseases, and diabetes, as it plays a critical role in signaling pathways associated with these conditions. -
GSK-3β Inhibitor
TCS2002 is a potent and selective inhibitor of GSK-3β, demonstrating an IC50 of 35 nM. This compound exhibits favorable pharmacokinetic properties, including efficient blood-brain barrier penetration. TCS2002 is valuable for research related to Alzheimer’s disease and the investigation of associated neurodegenerative mechanisms. -
GSK-3 Inhibitor
BIP-135 is a selective ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3) with IC50 values of 16 nM for GSK-3α and 21 nM for GSK-3β. This compound demonstrates neuroprotective effects, making it a valuable tool in research focused on neurodegenerative diseases and related pathways. Its specificity and potency position BIP-135 as a significant reagent for studying GSK-3-related biological processes. -
GSK-3/CDK2/CDK5 Inhibitor
GSK-3 Inhibitor 4 is a potent inhibitor of Glycogen Synthase Kinase 3 (GSK-3), Cyclin-Dependent Kinase 2 (CDK2), and Cyclin-Dependent Kinase 5 (CDK5), demonstrating IC50 values of 0.56 nM for GSK-3β, 0.45 nM for GSK-3α, 0.47 μM for CDK2, and 0.68 μM for CDK5. This compound effectively attenuates the phosphorylation of Tau protein, making it a valuable tool for investigating mechanisms underlying Alzheimer's disease. Its oral bioavailability and ability to penetrate the blood-brain barrier further enhance its utility in neuropharmacological research. -
GSK-3β Inhibitor
GSK-3β inhibitor 10 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 80.5 nM. This compound is valuable for studies investigating the role of GSK-3β in various neurodegenerative disorders, particularly Alzheimer’s disease. Its inhibitory action on GSK-3β may contribute to understanding the molecular mechanisms underlying these conditions and aid in the development of targeted therapeutic strategies. -
GSK-3
5-Bromo-3-indoxylacetate is a potent inhibitor of glycogen synthase kinase 3 (GSK-3) with a reported pIC50 of 3.39. This compound exhibits significant biological activity, making it a valuable tool for research focused on signal transduction pathways involved in various diseases, including cancer and neurodegenerative disorders. Its inhibitory effects on GSK-3 can be utilized to explore cellular processes such as glycogen metabolism, cell differentiation, and proliferation. -
GSK3 Inhibitor
(R)-BRD3731 is a selective glycogen synthase kinase 3 (GSK3) inhibitor. It demonstrates inhibitory activity with IC50 values of 1.05 μM for GSK3β and 6.7 μM for GSK3α. This compound is utilized in research focused on understanding GSK3's role in various cellular processes and diseases, including diabetes, neurodegenerative disorders, and cancer. As a valuable tool for studying GSK3 modulation, (R)-BRD3731 facilitates the exploration of therapeutic strategies that target this kinase. -
GSK-3β Inhibitor
GSK-3β Inhibitor 11 is a specific inhibitor of glycogen synthase kinase-3β (GSK-3β) with an IC50 value of 10.02 μM. This compound plays a significant role in modulating signaling pathways involved in neurodegenerative diseases, making it a valuable tool for research in this area. Its ability to selectively inhibit GSK-3β enables investigations into its potential therapeutic effects on associated pathological mechanisms. -
GSK3 Inhibitor
GSK3-IN-9 is a selective inhibitor of glycogen synthase kinase 3 (GSK3). This compound exhibits notable biological activity in neurodevelopmental and psychiatric disorders, including Fragile X syndrome and attention deficit hyperactivity disorder (ADHD). Additionally, GSK3-IN-9 shows potential applicability in research related to childhood seizures, intellectual disabilities, diabetes, acute myeloid leukemia (AML), autism, and other psychiatric disorders. -
GSK3 Inhibitor
GSK3-IN-2 is a potent inhibitor of glycogen synthase kinase 3 (GSK3), a key regulator of various cellular processes, including metabolism, cell differentiation, and apoptosis. This compound selectively inhibits GSK3 activity, leading to increased levels of β-catenin and modulation of Wnt signaling pathways. GSK3-IN-2 is valuable for research in cancer biology, neurodegenerative diseases, and regenerative medicine, where GSK3's role in cellular signaling and function is of significant interest. -
GSK-3
BRD5648 serves as a negative control for the potent GSK-3α inhibitor, BRD0705. This compound selectively targets GSK-3α with an IC50 of 66 nM, demonstrating up to an 8-fold preference over GSK-3β, which has an IC50 of 515 nM. Research applications for BRD5648 include investigations into mechanisms of action for GSK-3 inhibition, particularly in the context of acute myeloid leukemia (AML) and related hematological malignancies. -
GSK3 inhibitor
GS87 is a selective GSK3 inhibitor, demonstrating IC50 values of 415 nM for GSK3α and 521 nM for GSK3β. It effectively activates GSK3-dependent signaling pathways, including MAPK signaling, leading to differentiation of acute myeloid leukemia (AML) cell lines. GS87 exhibits superior modulation of key GSK3 target proteins associated with cell proliferation and differentiation compared to alternative GSK3 inhibitors. This compound holds promise as a differentiation agent for research involving non-promyelocytic AML. -
GSK-3b Inhibitor
GSK3β-IN-1 is a potent inhibitor of glycogen synthase kinase-3β (GSK-3β), with an IC50 value of 65 nM. This compound plays a crucial role in the modulation of key signaling pathways involved in neuronal function and is particularly relevant in the context of Alzheimer's disease research. Its application extends to investigating GSK-3β's involvement in various cellular processes and potential therapeutic strategies for neurodegenerative disorders. -
TbGSK3 Inhibitor
Antitrypanosomal agent 14 is a selective inhibitor of TbGSK3, demonstrating an IC50 of 12 μM and an EC50 of 0.47 μM against Trypanosoma brucei. This compound is primarily utilized in research focused on Human African trypanosomiasis, aiding in the exploration of therapeutic strategies against this parasitic infection. Its targeted mechanism suggests potential for further studies in drug development and disease management. -
CK1γ/GSK3β Inhibitor
AKI-062a is a non-selective inhibitor targeting CK1γ and GSK3β, key regulators in the WNT signaling pathway. It exhibits an ability to modulate various kinase activities, binding to 17 kinases at 1 μM concentration, with a relative activity of less than 10% compared to controls. This compound is valuable for research applications related to cell signaling, cancer biology, and developmental processes where WNT signaling is involved.
