Catalog No.
Product Name
Application
Product Information
Citations
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GSK-3 Substrate
2B-(SP) is an eIF2B-based substrate specifically designed for glycogen synthase kinase-3 (GSK-3). It exhibits efficient phosphorylation by both GSK-3α and GSK-3β isoforms, making it a valuable tool for studying GSK-3-related signaling pathways and cellular processes. This compound is suitable for research applications involving protein phosphorylation and GSK-3 activity modulation. -
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. -
GSK-3β/α Inhibitor
MJ34 is a potent inhibitor of glycogen synthase kinase-3 beta (GSK-3β) and alpha (GSK-3α), exhibiting IC50 values of 15.4 nM and 31.5 nM, respectively. This compound is critical for studies investigating the role of GSK-3 in cancer biology, including cellular signaling pathways and disease progression. MJ34’s ability to selectively inhibit these kinases makes it a valuable tool for exploring therapeutic strategies in cancer research. -
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. -
GSK-3α Inhibitor
(Rac)-BRD0705 is a racemic mixture that functions as a selective inhibitor of GSK-3α, exhibiting an IC50 of 66 nM and a Kd of 4.8 μM. This compound demonstrates a notable selectivity for GSK-3α, being eight times more potent than for GSK-3β, which has an IC50 of 515 nM. (Rac)-BRD0705 is relevant for research applications involving acute myeloid leukemia (AML) and other conditions where GSK-3 inhibition may play a critical role in disease mechanisms. -
GSK-3β Inhibitor
TC-G 24 is a selective glycogen synthase kinase-3β (GSK-3β) inhibitor, exhibiting an IC50 of 17.1 nM. This compound is capable of crossing the blood-brain barrier, making it valuable for research on various neurological and metabolic disorders, including type 2 diabetes mellitus, stroke, and Alzheimer's disease. TC-G 24 offers a useful tool for investigating the therapeutic potential of GSK-3β modulation in relevant disease models. -
GSK-3β Inhibitor
GSK-3β inhibitor 17 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β). This compound demonstrates a capacity to reduce cisplatin-induced phosphorylation of p65 and the expression of KIM-1 protein and mRNA. Additionally, GSK-3β inhibitor 17 effectively lowers the mRNA levels of pro-inflammatory cytokines such as TNF-α, IL-1β, IL-6, and MCP-1. It exhibits anti-inflammatory properties and holds promise for research into acute kidney injury. -
GSK-3 Substrate
Phospho-Glycogen Synthase Peptide-2 is a specific substrate for glycogen synthase kinase-3 (GSK-3). This peptide facilitates the study of GSK-3 activity and its role in various signaling pathways. It is also suitable for affinity purification of protein-serine kinases, enabling researchers to investigate kinase interactions and functions in cellular processes. -
hAChE/hBuChE Inhibitor
hAChE-IN-5 is a potent inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting IC50 values of 0.17 μM for both enzymes. In addition, hAChE-IN-5 demonstrates significant GSK3β inhibition with an IC50 of 0.21 μM. This compound is utilized in research focused on tau protein aggregation and Aβ1-42 self-aggregation, effectively preventing Aβ-dependent neurotoxicity. Furthermore, hAChE-IN-5 can cross the blood-brain barrier, showcasing its potential as a multi-targeted agent in the study of Alzheimer's disease. -
GSK-3β inhibitor
GSK-3β inhibitor 20 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 74.4 nM. This compound is primarily utilized in research applications aimed at understanding the role of GSK-3β in various signaling pathways, including those involved in metabolism, neurodegenerative diseases, and cancer. Its effective inhibition can provide insights into GSK-3β functions and facilitate the development of therapeutic strategies targeting this kinase. -
GSK-3β Inhibitor
18BIOder is a selective inhibitor of Glycogen Synthase Kinase 3 beta (GSK-3β) with notable neuroprotective properties. This compound has demonstrated efficacy in inhibiting HIV-1, contributing to its potential therapeutic applications in neurodegenerative diseases and HIV research. 18BIOder serves as a valuable tool for understanding the mechanistic pathways involved in GSK-3β modulation and its effects on cell signaling. -
GSK-3 Inhibitor
GSK-3 Inhibitor 6 is a potent inhibitor of glycogen synthase kinase 3 (GSK-3), displaying IC50 values of 29 nM for GSK-3α and 24 nM for GSK-3β. This compound demonstrates effective central nervous system penetration, making it suitable for neurological research. It is beneficial for studying GSK-3-related pathways in various biological contexts, including cell signaling and neurodegenerative disease models. -
GSK-3β Inhibitor
JGK-263 is an orally active inhibitor of Glycogen synthase kinase-3β (GSK-3β). It demonstrates neuroprotective properties and has the potential to enhance motor function. This compound is suitable for research applications related to neurological disorders, including amyotrophic lateral sclerosis (ALS). -
GSK-3 Inhibitor
PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3), a key regulator in various cellular processes. This compound exhibits antioxidant and metal-chelating properties, contributing to its potential applications in neuroprotection. Research indicates that PIMPC may offer therapeutic benefits in conditions such as Alzheimer's disease, making it a valuable tool for studies focused on neurodegenerative disorders and GSK-3 modulation. -
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. -
GSK-3β Inhibitor
GSK-3β Inhibitor 14 is a benzothiazepinone derivative that acts as a weak inhibitor of glycogen synthase kinase 3 beta (GSK-3β), with an IC50 greater than 100 μM. This compound is utilized in research focusing on GSK-3β-related pathways, potentially contributing to studies in various diseases, including neurodegenerative disorders and metabolic conditions. Its role in modulating GSK-3β activity makes it a valuable tool for elucidating the physiological and pathological functions associated with this important kinase. -
GSK-3β Inhibitor
ZDWX-25 is a potent dual inhibitor of GSK-3β and DYRK1A, demonstrating an IC50 value of 71 nM for GSK-3β. This compound exhibits significant cytotoxic effects on SH-SY5Y and HL-7702 cell lines, making it a valuable tool for research in neurodegenerative diseases such as Alzheimer's disease. Its inhibitory action on key kinase pathways suggests potential for further exploration in therapeutic applications. -
GSK-3β/CDK-2/CDK-4 Inhibitor
UNC10112785 is a potent inhibitor of serine/threonine kinases, specifically targeting GSK-3β, CDK-2, and CDK-4 with IC50 values of 0.031 μM, 0.016 μM, and 1.99 μM, respectively. This compound exhibits significant biological activity that positions it as a valuable tool in the study of type 2 diabetes. Its ability to modulate key pathways involved in metabolic regulation makes it an essential reagent for researchers investigating therapeutic interventions in diabetic conditions. -
GSK-3 Inhibitor
BRD1652 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3), a critical regulator in various signaling pathways. This compound has shown potential in modulating GSK-3 activity, making it a valuable tool for investigating the molecular mechanisms underlying emotion-related disorders. Its application can enhance research on neuropsychiatric conditions and therapeutic strategies targeting GSK-3 signaling. -
GSK-3β Inhibitor
Dihydronarwedine is an inhibitor of glycogen synthase kinase-3β (GSK-3β). At a concentration of 10 μM, it demonstrates a 39% reduction in GSK-3β activity. This compound is useful in research applications related to cellular signaling pathways, neurodegenerative diseases, and cancer therapy, where GSK-3β modulation is of interest. -
GSK-3 Inhibitor
GSK-3 inhibitor 7 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3), a key regulator in various cellular processes. This compound demonstrates significant activity in modulating GSK-3 signaling pathways, making it a valuable tool for research in neurobiology and related fields. Its application may enhance understanding of GSK-3's role in neurodegenerative diseases and neuronal signaling. -
GSK-3 Inhibitor
Cazpaullone is a potent glycogen synthase kinase-3 (GSK-3) inhibitor that plays a critical role in cellular signaling pathways. It enhances pancreatic beta cell protection and promotes their replication, making it valuable in diabetes research. Cazpaullone's mechanism of action provides insights into potential therapeutic strategies for diabetes and related metabolic disorders. -
GSK-3β Inhibitor
GSK-3β inhibitor 25 primarily targets glycogen synthase kinase 3 beta (GSK-3β), demonstrating weak inhibitory activity with an IC50 greater than 100 μM. This compound is utilized in biochemical research to elucidate the role of GSK-3β in various signaling pathways and cellular processes, including metabolism and cell proliferation. Its modest potency may serve as a lead in the development of more selective GSK-3β inhibitors for therapeutic applications. -
GSK-3β Inhibitor
GSK-3β inhibitor 26 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 18.23 μM. This compound is instrumental in research focusing on cancer, inflammation, and neurodegenerative diseases, facilitating the exploration of therapeutic pathways and mechanisms associated with GSK-3β modulation. -
GSK-3β Inhibitor
TD114-2 is a potent and highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β), exhibiting an IC50 value of 48 nM. The compound forms a key hydrogen bond with arginine 141, which contributes to its remarkable specificity for GSK-3β compared to other kinases. TD114-2 is a valuable tool for investigating the role of GSK-3β in various conditions, including diabetes, neurodegenerative diseases, and other disorders linked to GSK-3β dysregulation. -
PI4Kβ/PKG Inhibitor
PI4Kβ/PKG-IN-2 is a potent dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). This compound demonstrates significant inhibitory activity against Plasmodium, making it a valuable tool for investigating malaria pathogenesis and potential therapeutic strategies. Its oral bioavailability further supports its use in preclinical studies aimed at understanding malaria biology. -
PfGSK3/PfPK6 Inhibitor
PfGSK3/PfPK6-IN-1 is a selective inhibitor targeting PfGSK3 and PfPK6, with IC50 values of 97 nM and 8 nM, respectively. This compound effectively inhibits the proliferation of blood-stage Plasmodium falciparum 3D7 parasites, making it a valuable tool for malaria research. Additionally, PfGSK3/PfPK6-IN-1 exhibits low cytotoxicity in hepatocyte cultures at concentrations up to 200 nM, with a significant reduction in cell viability observed at 2 μM. Its dual action enhances its potential in studying malaria-related mechanisms and potential therapeutic strategies. -
Akt Inhibitor
Miransertib mesylate is a potent and selective allosteric inhibitor of the Akt family, demonstrating IC50 values of 2.7 nM, 14 nM, and 8.1 nM for Akt1, Akt2, and Akt3, respectively. This compound is particularly effective against the AKT1-E17K mutant variant, making it valuable for investigating PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib mesylate has shown efficacy against Leishmania, highlighting its versatility in biological research applications. -
PI4KA Inhibitor
PI4KA-IN-1 is a potent inhibitor of phosphatidylinositol 4-kinase alpha (PI4KA). This compound is valuable for studying the role of PI4KA in cellular processes and its implications in hepatitis C virus infection. By downregulating PI4KA activity, PI4KA-IN-1 can aid in elucidating the mechanisms of viral replication and pathogenesis, making it a useful tool for related therapeutic research and development. -
PI4KIIIα Inhibitor
AZD2836 is a selective inhibitor of the host cell kinase PI4KIIIα. By targeting this kinase, AZD2836 disrupts the metabolism of phosphatidylinositol 4-phosphate (PI4P), a crucial component for the replication of hepatitis C virus (HCV). In studies using HCV subgenomic replicon cell lines, AZD2836 demonstrated effective antiviral activity, exhibiting EC50 values of 270 nM for genotype 1b (Con1 strain) and 550 nM for genotype 1a (Lemon strain). This compound serves as a valuable tool for researching viral replication mechanisms and assessing therapeutic options for HCV. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-2 is a potent inhibitor targeting both MEK and PI3K pathways, exhibiting IC50 values of 352 nM for MEK1, 107 nM for PI3Kα, and 137 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT and ERK1/2, demonstrating significant anti-proliferative activity against various tumor cell lines. MEK/PI3K-IN-2 is valuable for research in cancer biology and therapeutic development aimed at disrupting these critical signaling pathways. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-1 is a potent inhibitor targeting MEK and PI3K pathways, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT (pAKT) and ERK1/2 (pERK1/2), demonstrating significant anti-proliferative effects in various tumor cell lines. MEK/PI3K-IN-1 serves as a valuable tool for research in cancer therapeutics and signaling pathway analysis. -
Akt Kinase Inhibitor
ML-9 Free Base is a selective and potent inhibitor of Akt kinase, demonstrating significant inhibitory effects on myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). It effectively inhibits MLCK, protein kinase A (PKA), and protein kinase C (PKC) with Ki values of 4 μM, 32 μM, and 54 μM, respectively. Additionally, ML-9 Free Base promotes autophagy by enhancing autophagosome formation while inhibiting their subsequent degradation, making it valuable for research on cellular signaling pathways and autophagic processes. -
AMPK Inhibitor
BAY-3827 is a potent and selective inhibitor of AMP-activated protein kinase (AMPK), exhibiting IC50 values of 1.4 nM at low ATP concentrations (10 μM) and 15 nM at higher ATP concentrations (2 mM). This compound demonstrates over 500-fold selectivity against a wide array of kinases, making it a valuable tool for elucidating AMPK-related pathways. BAY-3827 effectively inhibits the phosphorylation of acetyl-CoA carboxylase 1 and displays significant anti-proliferative effects in androgen-dependent prostate cancer cell lines, supporting its application in cancer research and metabolic studies. -
AMPK Inhibitor
AMPK-IN-3 is a potent and selective inhibitor of AMP-activated protein kinase (AMPK), exhibiting IC50 values of 60.7 nM for AMPK α2, 107 nM for AMPK α1, and 3820 nM for KDR. This compound effectively inhibits AMPK without impacting cell viability or inducing significant cytotoxicity in K562 cells. AMPK-IN-3 is valuable for research focused on cancer biology and the role of AMPK in metabolic regulation and cellular energy homeostasis. -
AMPK Activator
PF-739 is a potent and orally active activator of AMP-activated protein kinase (AMPK). It effectively stimulates 12 heterotrimeric AMPK complexes, leading to a significant reduction in plasma glucose levels. This compound is utilized in research to investigate metabolic disorders and the cellular responses to energy stress. Its role as a non-selective AMPK activator makes it a valuable tool in studies focused on cellular metabolism and energy homeostasis. -
AMPK Activator
Lixumistat acetate is a potent activator of AMP-activated protein kinase (AMPK), promoting increased phosphorylation of AMPK. This compound has demonstrated the ability to mitigate aging-related cognitive decline in animal models. Additionally, Lixumistat acetate acts as a strong inhibitor of oxidative phosphorylation (OXPHOS), making it a valuable tool for research in solid tumor applications. -
AMPK Inhibitor
Chromium(III) acetate functions as an AMPK inhibitor by inhibiting the phosphorylation of AMP-activated protein kinase (AMPK), subsequently promoting lipogenesis. This compound exhibits low toxicity in mammalian models, demonstrated by an LD50 of 2365 mg/kg in rats. It is primarily utilized in research to explore metabolic pathways and the regulation of energy homeostasis. -
AMPK Activator
PXL770 is a selective allosteric activator of AMP-activated protein kinase (AMPK) that enhances metabolic regulation. It has been shown to decrease very long-chain fatty acid (VLCFA) levels, improve mitochondrial respiration, and modulate gene expression in proinflammatory pathways in fibroblasts and lymphocytes related to X-linked adrenoleukodystrophy (ALD). In animal models, PXL770 normalizes plasma VLCFA levels and improves metabolic parameters such as glycemia and insulin sensitivity in diet-induced obesity. This compound serves as a valuable tool for research into ALD, autosomal dominant polycystic kidney disease, and nonalcoholic steatohepatitis (NASH). -
AMPK Activator
MOTS-c (mouse) is a mitochondrial-derived polypeptide that acts as an AMPK activator. It has been shown to modulate pancreatic cell function by reducing insulin secretion and expression in INS-1E cells, while enhancing glucagon secretion in αTC-1 cells. Additionally, MOTS-c (mouse) is effective in decreasing apoptosis in both INS-1E and αTC-1 cell lines. Its ability to counteract diet-induced obesity and insulin resistance highlights its potential in metabolic research. -
AMPK Activator
ZLN024 hydrochloride is an allosteric activator of AMP-activated protein kinase (AMPK). It selectively activates various AMPK heterotrimers, including AMPK α1β1γ1, α2β1γ1, α1β2γ1, and α2β2γ1, with EC50 values of 0.42 µM, 0.95 µM, 1.1 µM, and 0.13 µM, respectively. This compound is instrumental in studies related to energy homeostasis, metabolism, and cellular stress response, making it a valuable tool for researchers investigating AMPK-related pathways in various biological contexts. -
AMPK/Nrf2 Activator
Fortunellin is a flavonoid that acts as an AMPK/Nrf2 activator, derived from the fruits of Fortunella margarita (kumquat). It demonstrates minimal toxicity in murine models and effectively reduces inflammation and reactive oxygen species (ROS) generation in H9C2 cells induced by lipopolysaccharide (LPS). By enhancing the AMPK/Nrf2 pathway, Fortunellin protects against fructose-induced inflammation and oxidative stress, making it a valuable tool for research in diabetic cardiomyopathy. -
AMPK Inhibitor
AMPK-IN-4 is a selective inhibitor of AMP-activated protein kinase (AMPK), targeting both AMPKα1 and AMPKα2 with IC50 values of 393 nM and 141 nM, respectively. This compound is significant in cancer research, facilitating investigations into metabolic regulation and cellular energy homeostasis. Its efficacy in modulating AMPK activity makes it a valuable tool for studying the pathways associated with tumor metabolism and potential therapeutic strategies. -
AMPK Activator
PT1 is an activator of AMPKα1, specifically designed to directly activate the inactive truncated forms of AMPKα1 monomers. This compound enhances AMPK signaling, which plays a critical role in cellular energy homeostasis and metabolism. PT1 is valuable for research applications investigating metabolic disorders, cellular response to stress, and the regulatory mechanisms of energy balance. -
AMPK Substrate
SAMS peptide is a specific substrate for AMP-activated protein kinase (AMPK), facilitating the investigation of AMPK activation and its downstream signaling pathways. This peptide plays a critical role in metabolic research, allowing for the study of energy homeostasis and cellular responses to stress. SAMS is essential for probing the physiological effects of AMPK modulation in various biological contexts. -
AMPK Activator
Lixumistat hydrochloride is a potent AMPK activator that increases AMPK phosphorylation, thereby modulating critical metabolic pathways. This compound has been shown to mitigate aging-associated cognitive impairment in animal models, making it a valuable tool in neurobiology research. Additionally, Lixumistat hydrochloride acts as an effective oxidative phosphorylation (OXPHOS) inhibitor, relevant for studies focusing on solid tumors. -
AMPK Activator
PF-06685249 is a potent allosteric activator of AMP-activated protein kinase (AMPK), exhibiting an EC50 of 12 nM for recombinant AMPK α1β1γ1. This compound has demonstrated efficacy in enhancing renal function in ZSF-1 rats with diabetic nephropathy. PF-06685249 is suitable for research applications targeting metabolic diseases and diabetic nephropathy. -
AMPK Activator
COH-SR4 is a potent AMPK activator that exhibits significant anti-proliferative effects against various cancers, including leukemia, melanoma, breast, and lung cancers. By activating AMPK, COH-SR4 inhibits adipocyte differentiation, making it a valuable tool for studying obesity and related metabolic disorders. This compound is crucial for research aimed at understanding metabolic regulation and the therapeutic potential of targeting AMPK in cancer and metabolic diseases. -
AMPK Activator
Ampkinone is an indirect activator of AMP-activated protein kinase (AMPK), targeting metabolic pathways involved in energy homeostasis. It enhances AMPK activity, which plays a crucial role in regulating cellular energy balance, glucose uptake, and lipid metabolism. This compound is valuable in research applications focused on metabolic disorders, obesity, and diabetes, offering insights into therapeutic strategies for these conditions.
