GSK-3

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  1. GSK-3β Inhibitor

    Manzamine A hydrochloride is an orally active beta-carboline alkaloid that specifically inhibits GSK-3β and CDK-5, with IC50 values of 10.2 μM and 1.5 μM, respectively. This compound demonstrates significant antimalarial and anticancer properties, with additional effects such as inhibiting vacuolar ATPases and autophagy processes in pancreatic cancer cells. Furthermore, Manzamine A hydrochloride exhibits potent activity against HSV-1, making it valuable for various research applications in cancer biology and virology.
  2. GSK-3β Inhibitor

    GSK-3β inhibitor 13 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and GSK-3α, demonstrating IC50 values of 0.73 nM and 0.35 nM respectively. This orally active compound exhibits blood-brain barrier permeability and effectively reduces tau phosphorylation, with an IC50 of 58 nM. Its ability to modulate tau phosphorylation makes it valuable for research focused on neurodegenerative disorders, particularly Alzheimer's disease, by potentially mitigating the formation of neurofibrillary tangles.
  3. CDK/GSK3β/JNK Inhibitor

    Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. CDK/GSK-3 Inhibitor

    CDK5-IN-4 is a potent multikinase type-II inhibitor primarily targeting cyclin-dependent kinase 5 (CDK5), with an IC50 of 9.8 μM. Additionally, it exhibits inhibitory activity against GSK-3α and GSK-3β with IC50 values of 0.98 μM and 4.00 μM, as well as CDK9 and CDK2, with IC50 values of 1.76 μM and 6.24 μM, respectively. This compound is particularly relevant for research on glioblastoma and may aid in understanding its molecular mechanisms.
  44. AChE/BACE1/GSK3β Inhibitor

    AChE/BACE1/GSK3β-IN-1 is a potent triple inhibitor targeting acetylcholinesterase (AChE), beta-secretase 1 (BACE1), and glycogen synthase kinase 3 beta (GSK3β). It demonstrates effective inhibitory activity with IC50 values of 1.0 μM for AChE, 20 μM for BACE1, and 15 μM for GSK3β. With favorable blood-brain barrier penetrability and bioavailability, AChE/BACE1/GSK3β-IN-1 is a valuable tool for research into Alzheimer's disease mechanisms and therapeutics.
  45. AChE/GSK-3β Inhibitor

    ZLWH-23 is a selective inhibitor of acetylcholinesterase (AChE) with an IC50 of 0.27 μM and also inhibits glycogen synthase kinase-3 beta (GSK-3β) with an IC50 of 6.78 μM. It exhibits greater selectivity for AChE compared to butyrylcholinesterase (BChE) and shows preferential inhibition of GSK-3β over a range of multi-kinases. This compound is relevant for research focused on Alzheimer's disease pathophysiology.
  46. GSK-3β Inhibitor

    GSK-3β Inhibitor 12 is a selective inhibitor of glycogen synthase kinase-3 beta (GSK-3β), demonstrating a significant reduction in enzymatic activity by 49.11% at 25 μM and 37.11% at 50 μM concentrations. This compound is valuable for research into neurodegenerative diseases, providing insights into GSK-3β's role in cellular processes and disease mechanisms. Its application may facilitate the development of therapeutic strategies targeting GSK-3β-related pathways.
  47. 3F8

    GSK-3β inhibitor

    3F8 is a potent and selective inhibitor of glycogen synthase kinase-3 beta (GSK-3β). It demonstrates significant biological activity in modulating GSK-3β signaling pathways, making it a valuable tool for research into various GSK-3β associated diseases, including neurodegeneration and cancer. This compound holds potential as a therapeutic candidate, offering insights into the regulatory roles of GSK-3β in cellular processes.
  48. GSK-3 Inhibitor

    CHIR-21208 is a highly selective inhibitor of glycogen synthase kinase-3 (GSK-3), a critical regulator in various cellular processes. This compound demonstrates significant potential in the study of neurodegenerative diseases, including Alzheimer's disease, as well as metabolic disorders such as type 2 diabetes. Researchers can utilize CHIR-21208 to explore GSK-3's role in signaling pathways and its implications in disease mechanisms.
  49. AChE/GSK-3β Inhibitor

    PJ17 is a potent dual inhibitor of acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), exhibiting IC50 values of 8.84 μM and 4.19 μM, respectively. This compound demonstrates a lack of significant neurotoxicity in primary cerebellar granule neuron cultures, making it a promising candidate for neuropharmacological studies. PJ17 serves as a valuable template for the development of multitarget therapeutics and is relevant in research focused on Alzheimer's disease.
  50. GSK-3 Inhibitor

    GSK3-IN-11 is a selective inhibitor of Glycogen Synthase Kinase-3 (GSK-3), exhibiting an IC50 of 5010 nM. This compound plays a critical role in regulating various cellular processes, including glycogen metabolism, cell cycle progression, and apoptosis. GSK3-IN-11 is utilized in research to study GSK-3-related signaling pathways and its implications in diseases such as diabetes, cancer, and neurodegenerative disorders.

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