Catalog No.
Product Name
Application
Product Information
Citations
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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. -
AKT1/MAPK1 Ligand
N-Acetyldehydroanonaine is a natural alkaloid that functions as a ligand for AKT1 and MAPK1, key regulators in various signaling pathways. This compound, derived from plants of the Zanthoxylum genus, exhibits potential biological activity relevant to cancer research. Its application is particularly significant in the study of diseases such as gastric cancer, making it a valuable tool for investigators exploring therapeutic targets and mechanisms in oncogenesis. -
MAPK/PI3K Antagonist
ST-162 is a dual antagonist of the MAPK and PI3K signaling pathways. It demonstrates significant antitumor activity and has been shown to enhance the efficacy of immune checkpoint inhibitors. This compound is suitable for cancer research, particularly in the study of melanoma and other malignancies. -
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. -
AMPK Activator
Foenumoside B is a triterpene saponin that activates AMP-activated protein kinase (AMPK) signaling. This compound inhibits PPARγ-induced adipogenesis and promotes lipid metabolism shift towards lipolysis. Foenumoside B is useful for investigating obesity and related metabolic disorders, making it a valuable tool for research in metabolic health. -
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. -
AMPK Activator
IMM-H007 is a potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. This compound exhibits cardioprotective effects by activating AMPK, which subsequently reduces endothelial inflammation through the inactivation of NF-κB and JNK/AP1 signaling pathways. Additionally, IMM-H007 regulates lipid metabolism, effectively resolving hepatic steatosis in high-fat diet-fed hamsters. It is suitable for research applications focused on nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis. -
AMPK Activator
AMPK Activator 18 is a potent allosteric activator of AMPK complexes, particularly those containing the β2 isoform. It effectively activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, exhibiting EC50 values of 17.2 nM and 82.1 nM, respectively. This compound stimulates β2-AMPK in cellular contexts and enhances glucose uptake in isolated skeletal muscle. Additionally, AMPK Activator 18 promotes phosphorylation of acetyl-coenzyme A carboxylase (ACC) and AMPK at the α-T172 site, making it a valuable tool for research in type 2 diabetes. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
GSK3 Inhibitor
GSK3-IN-4 is a potent glycogen synthase kinase 3 (GSK3) inhibitor, specifically designed to modulate GSK3 activity. This compound has demonstrated significant biological activity relevant to the study of psychiatric disorders, making it a valuable tool for exploring the molecular mechanisms underlying these conditions. GSK3-IN-4's inhibition of GSK3 opens avenues for therapeutic research and the development of novel treatments targeting neurological diseases. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
GSK3 Inhibitor
CHIR-98023 is a selective and reversible inhibitor of glycogen synthase kinase 3 (GSK3), demonstrating IC50 values of 10 nM for GSK3α and 6.7 nM for GSK3β. This compound enhances insulin signaling and glucose metabolism, making it valuable for research in diabetes and metabolic disorders. Its specificity for GSK3 further supports its potential in elucidating the pathways associated with cell signaling and energy homeostasis. -
GSK3β Inhibitor
GSK3β-IN-4 is a potent and selective ATP-competitive inhibitor of GSK3β, exhibiting an IC50 of 0.37 nM. This compound also shows activity against GSK3α with an IC50 of 2.75 nM and a selectivity index of 7.4. GSK3β-IN-4 effectively reduces tau phosphorylation at Ser396 and has demonstrated improvements in cognitive deficits in Alzheimer's disease models. It is suitable for research focused on Alzheimer's disease pathophysiology and potential therapeutic interventions. -
CDK/GSK3 Inhibitor
Aloisine RP106 is a potent inhibitor of cyclin-dependent kinases (CDKs) Cdk1/cyclin B and Cdk5/p25, as well as glycogen synthase kinase 3 (GSK3), with IC50 values of 0.70 µM, 1.5 µM, and 0.92 µM, respectively. This compound is valuable for research applications targeting cell cycle regulation and neurodegenerative diseases, where CDK and GSK3 activity contribute to pathological processes. Researchers can utilize Aloisine RP106 to investigate the role of these kinases in various biological contexts including cancer and neurobiology. -
PfGSK3/PfPK6 Inhibitor
PfGSK3/PfPK6-IN-2 is a potent dual inhibitor of PfGSK3 and PfPK6, with IC50 values of 172 nM and 11 nM, respectively. This compound exhibits significant efficacy in the modulation of key signaling pathways in Plasmodium falciparum, making it a valuable tool for malaria research. Its ability to inhibit these targets can aid in the investigation of therapeutic strategies against malaria. -
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. -
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. -
AMPK Activator
Galegine hemisulfate is a guanidine derivative that functions as an AMPK activator. It has demonstrated potential in promoting weight loss in mice and effectively activates AMPK in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, Galegine hemisulfate exhibits antibacterial properties, with a minimum inhibitory concentration of 4 mg/L against strains of Staphylococcus aureus, making it relevant for various biological research applications. -
AMPK Activator
Galegine hydrochloride is an AMPK activator that influences energy metabolism and contributes to weight management. Derived from the guanidine structure, this compound has shown efficacy in activating AMPK in various cell lines, including 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cells. Additionally, galegine hydrochloride exhibits antibacterial properties, demonstrating a minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains, highlighting its potential in metabolic and antimicrobial research applications. -
ATR Inhibitor
ATR-IN-31 is a selective ATR kinase inhibitor that exhibits an IC50 of 7 nM, demonstrating its potent activity. This compound functions by specifically inhibiting ATR kinase activity without significantly affecting ATM kinase. ATR-IN-31 has shown efficacy in reducing the viability of prostate cancer cells, making it a valuable tool for research focused on prostate cancer. -
ATM/ DNA-PKcs Inhibitor
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms. -
ATR Substrate
ATR kinase substrate peptide (ASELPASQPQPFSAKKK) functions as a specific substrate for ATR protein kinase, facilitating the detection of ATR kinase activity in biological research. This peptide is instrumental in studying cellular responses to DNA damage and the associated signaling pathways. It plays a critical role in validating ATR kinase activity and exploring its implications in cancer biology and therapeutic development. -
ATR Inhibitor
(S)-Ceralasertib is an ATR inhibitor, specifically targeting ataxia telangiectasia mutated and rad3 related (ATR) signaling pathways. This compound exhibits significant potential in cancer research by enhancing the sensitivity of tumor cells to DNA-damaging agents through inhibition of the ATR pathway. (S)-Ceralasertib is utilized in studies aimed at understanding the roles of DNA repair mechanisms and evaluating combination therapies for various cancers. -
ATM Inhibitor
WSD0628 is a potent ATM inhibitor known for its ability to cross the blood-brain barrier. It exhibits significant radiosensitizing effects, making it a valuable tool for research in cancer therapy and radiobiology. Its inhibition of the ATM pathway has implications for enhancing the efficacy of radiotherapy in various malignancies. -
PROTAC ATR Degrader
PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies. -
ATM Inhibitor
M3541 is a potent, ATP-competitive inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 0.25 nM. This compound demonstrates significant selectivity against other protein kinases. M3541 effectively hinders the repair of double-strand breaks (DSB) and displays notable antitumor activity, making it a valuable tool for cancer research and therapeutic studies targeting DNA damage response pathways. -
ATM/ATR
SKLB-197 is a selective inhibitor of ATR (ATM and Rad3-related protein) with an IC50 value of 0.013 μM, demonstrating minimal activity against a panel of 402 other protein kinases. This compound exhibits significant antitumor efficacy specifically in ATM-deficient tumors, showing potent activity in both in vitro and in vivo models. SKLB-197 serves as a valuable tool for investigating the roles of ATM and ATR in cancer biology and for the development of targeted therapies. -
ATR Inhibitor
ATR-IN-4 is a selective inhibitor of the ATR (Ataxia Telangiectasia Mutated and Rad3-related) kinase. This compound exhibits significant antiproliferative activity against human prostate cancer cells (DU145) and human lung cancer cells (NCI-H460), yielding IC50 values of 130.9 nM and 41.33 nM, respectively. ATR-IN-4 is valuable for research investigating DNA damage response pathways and potential therapeutic strategies in cancer treatment. -
Atm Inhibitor
ATM Inhibitor-10 is a selective ATM inhibitor characterized as a 3-quinoline carboxamide with an IC50 of 0.6 nM. This compound demonstrates significant anti-tumor activity in SW620 xenograft models and shows synergistic effects when combined with Top I inhibitors. It serves as a valuable tool for studies involving DNA damage response and cancer therapeutics. -
PROTAC ATR Degrader
Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage.
