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Catalog No.
Product Name
Application
Product Information
Citations
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PI3Kα/HDAC6 Inhibitor
PI3Kα/HDAC6-IN-1 is a dual inhibitor targeting PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. This compound effectively inhibits AKT (Ser473) phosphorylation and promotes the accumulation of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. Its potent anti-cancer activity is demonstrated in the L-363 cell line with an IC50 of 0.17 μM, highlighting its potential for therapeutic applications in cancer research. -
PI3K Inhibitor
PI3K/HDAC-IN-1 is a potent dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC). It effectively inhibits PI3Kδ and HDAC1 with IC50 values of 8.1 nM and 1.4 nM, respectively. This compound is valuable for studying the roles of PI3K and HDAC in various cellular processes and can aid in cancer research by exploring the therapeutic potential of dual inhibition in tumor models. -
PI3Kδ Inhibitor
FD223 is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), demonstrating an IC50 of 1 nM. It shows significant selectivity over other isoforms, with IC50 values of 51 nM, 29 nM, and 37 nM for α, β, and γ, respectively. FD223 effectively inhibits the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473, leading to G1 phase arrest in the cell cycle. This compound holds potential for research into leukemia, particularly AML. -
mTOR Inhibitor
2,6-Dihydroxyacetophenone primarily functions as an mTOR inhibitor. This polyphenolic derivative exhibits significant antioxidant activity and effectively inhibits cell growth and proliferation in colorectal cancer (CRC) cells by inducing apoptosis and arresting the cell cycle at the G0/G1 phase, while also suppressing cell migration. Additionally, 2,6-Dihydroxyacetophenone inhibits xanthine oxidase with an IC50 of 1.24 mM and enhances uric acid metabolism in hyperuricemic models. It further reduces plasma cholesterol levels in hypercholesterolemic rats and mitigates lipid accumulation in mice subjected to a high-fat diet. This compound is valuable for research into CRC, hyperuricemia, and hypercholesterolemia. -
mTORC1/2 Inhibitor
(+)–Usnic acid is a potent mTORC1/2 inhibitor derived from lichens, acting by binding to the ATP-binding pocket of mTOR. It effectively inhibits the phosphorylation of downstream effectors such as Akt (Ser473), 4EBP1, and S6K, thereby promoting autophagy and exhibiting both anti-cancer and anti-inflammatory properties. Additionally, (+)-Usnic acid demonstrates antimicrobial activity against several planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium, making it a valuable tool for various biological research applications. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development. -
mTOR/HDAC Inhibitor
mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies. -
GSK-3β/G9a Inhibitor
GSK-3β/G9a-IN-1 is a selective inhibitor of GSK-3β and G9a, acting through competitive mechanisms with IC50 values of 0.8 μM and 1.1 μM, respectively. This compound is effective in lowering tau phosphorylation and reducing Aβ aggregation, making it relevant for Alzheimer's disease research. Additionally, GSK-3β/G9a-IN-1 influences chromatin dynamics by inhibiting H3K9me2 and modulating members of the SAGA complex. Its ability to improve memory and restore social behaviors highlights its potential as a therapeutic agent in neurodegenerative conditions. -
mTOR/p70s6K Inhibitor
Zederone is a sesquiterpene that acts as an inhibitor of the mTOR/p70S6K signaling pathway. It effectively reduces ovarian cancer cell proliferation and exhibits selective inhibition of various CYP450 enzymes, notably with IC50 values of 2.9 μM for CYP2B6 and 9.2 μM for CYP2C9. Additionally, Zederone demonstrates antibacterial properties against multi-drug resistant strains of Staphylococcus aureus and has been shown to improve cognitive function while modulating gut bacterial dysbiosis. However, caution is warranted due to its hepatotoxicity, evidenced by an LD50 of approximately 223 mg/kg in mice. -
PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator
JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms. -
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. -
PI3K/PIKK Inhibitor
PI3K/PIKK-IN-1 is a potent inhibitor of phosphoinositide 3-kinases (PI3K) and PI3-kinase-related kinases (PIKK). This compound is utilized in the development of antibody-drug conjugates (ADCs), making it valuable for therapeutic applications. It is particularly relevant in the research of various cancers, including breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer, aiding in the exploration of targeted cancer therapies. -
Akt/ROCK Inhibitor
Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development. -
PI3Kδ/BET Inhibitor
PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development. -
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. -
PI3Kα Inhibitor
PI3Kα-IN-16 is a selective PI3Kα inhibitor with an IC50 value of 4.28 μM. It effectively suppresses PI3K-mediated colorectal cancer growth and migration, demonstrating its potential as a therapeutic agent. Additionally, PI3Kα-IN-16 inhibits the Wnt signaling pathway, making it a valuable tool for research in cancer biology and signaling pathways. -
AMPK Inhibitor
AMPK activator 16 is a potent AMP-activated protein kinase (AMPK) activator that effectively enhances AMPK signaling. It promotes the phosphorylation of AMPK, subsequently increasing the levels of phosphorylated acetyl-CoA carboxylase (p-ACC) and phosphorylated raptor (p-raptor) in N2a cells. This compound is instrumental in studies exploring metabolic regulation and signaling pathways linked to energy homeostasis and cellular stress responses. -
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. -
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. -
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. -
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. -
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. -
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.
