Catalog No.
Product Name
Application
Product Information
Citations
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ATM Inhibitor
ATM Inhibitor-2 is a highly potent and selective inhibitor of ataxia telangiectasia mutated (ATM) kinase, exhibiting an IC50 of less than 1 nM. This compound is valuable in studying DNA damage response mechanisms and cell cycle regulation. Researchers can utilize this inhibitor to explore potential therapeutic strategies in cancer treatments and related biological pathways. -
ATR Inhibitor
ATR-IN-20 is a potent inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein) with an IC50 value of 3 nM. In addition to its primary action on ATR, ATR-IN-20 also inhibits mTOR with an IC50 of 18 nM while demonstrating selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). This compound shows a favorable pharmacokinetic profile with 30% oral bioavailability, indicating its potential for applications in anticancer research and therapeutic development. -
ATR Inhibitor
ATR-IN-8 is a potent inhibitor of ATR (ataxia telangiectasia and Rad3-related protein), a critical enzyme involved in the homologous recombination repair pathway and a member of the PIKK family. This compound demonstrates significant biological activity in disrupting ATR-mediated DNA damage response mechanisms, making it a valuable tool for cancer research. ATR-IN-8 can be utilized to investigate the therapeutic implications of ATR inhibition in various cancer models and studies related to DNA repair mechanisms. -
ATM Inhibitor
Antitumor agent-28 is a selective inhibitor of ataxia telangiectasia mutated (ATM) kinase. By inhibiting ATM activity, it disrupts DNA damage response pathways, demonstrating potent anti-cancer efficacy. This compound is valuable for research applications focused on cancer biology, DNA repair mechanisms, and therapeutic development. -
ATM Inhibitor
ATM-IN-12 is a specific inhibitor of ATM kinase, exhibiting an IC50 of 1.26 μM. This compound is instrumental in studying ATM kinase-mediated diseases, particularly in cancer research. By targeting ATM kinase, ATM-IN-12 provides valuable insights into the cellular responses to DNA damage and the mechanisms underlying tumorigenesis. -
ATR Kinase Inhibitor
ATR-IN-29 is a highly potent ATR kinase inhibitor, demonstrating an IC50 value of 1 nM. This compound exhibits significant antiproliferative activity, making it a valuable tool for investigating the role of ATR in cancer cell proliferation. ATR-IN-29 is ideal for studies focused on DNA damage response and cell cycle regulation, providing insights into therapeutic interventions for cancer treatment. -
ATR Inhibitor
ATR-IN-13 is a potent inhibitor of ATR kinase, exhibiting an IC50 of 2 nM. This compound is primarily utilized in research related to ATR kinase-mediated diseases, including proliferative disorders and various forms of cancer. Its specific inhibitory activity makes it a valuable tool for exploring the roles of ATR kinase in tumor biology and therapeutic interventions. -
ATM Kinase Inhibitor
ATM-IN-13 is a selective inhibitor of ATM kinase, exhibiting an IC50 of 0.3 nM in human cells. This compound effectively disrupts the ATM-mediated signaling pathway responsible for DNA double-strand break repair, resulting in decreased phosphorylation of ATM and p53 and inhibiting the ATM-dependent DNA damage response. ATM-IN-13 is a valuable tool for advancing research in colorectal cancer and understanding the mechanisms of DNA repair and cellular response to genotoxic stress. -
ATR Inhibitor
ATR-IN-18 is a potent and orally active ATR kinase inhibitor with an IC50 of 0.69 nM. It exhibits significant antiproliferative effects in LoVo cells, achieving an IC50 of 37.34 nM. Due to its inhibitory effects on ATR, ATR-IN-18 is relevant for research applications in cancer biology and therapeutic development. -
ATR Protein kinase Inhibitor
ATR kinase-IN-2 is a selective inhibitor of ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM. This compound is valuable for investigating the role of ATR in DNA damage response pathways and its implications in cancer biology. Research applications include exploring tumor cell sensitivity to DNA-damaging agents and elucidating mechanisms of resistance to cancer therapies. -
ATR Inhibitor
ATR-IN-5 is a potent inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein), a member of the PI3K-related kinase family that plays a crucial role in maintaining genome stability and facilitating DNA damage repair. This compound is valuable for research into ATR kinase-mediated diseases, including various proliferative disorders and cancers. Its inhibitory effects on ATR provide a useful tool for investigating therapeutic strategies targeting DNA repair mechanisms in these conditions. -
ATM/ATR Inhibitor
ATM Inhibitor-9 is a selective inhibitor targeting ATM kinase, with an IC50 value of 5 nM. It effectively impairs ATM-mediated signaling pathways, making it an invaluable tool for cancer research, particularly in studies involving DNA damage response and repair mechanisms. This compound can be used to explore the role of ATM in tumor biology and therapeutic resistance. -
ATM Inhibitor
ATM Inhibitor-8 is a selective and potent inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 1.15 nM. This compound demonstrates significant anti-tumor activity, making it valuable for research in cancer biology and therapeutic development. Its oral bioavailability enhances its utility in in vivo studies exploring the role of ATM inhibition in various malignancies. -
ATR Protein Kinase Inhibitor
ATR kinase-IN-3 is a potent ATR protein kinase inhibitor with a Ki value ranging from 0.01 to 1 μM. This compound significantly modulates the ATR signaling pathway, making it valuable for studies in cancer biology, particularly in understanding DNA damage response mechanisms. Its ability to inhibit ATR activity can aid in assessing the therapeutic potential of targeting this pathway in various cancer models. -
ATR Inhibitor
ATR-IN-16 is a potent inhibitor of the ATR kinase, a critical regulator of the DNA damage response pathway. This compound demonstrates significant anticancer activity, exhibiting an IC50 of 410 nM in LoVo cells. ATR-IN-16 is applicable in cancer research, particularly for studies focused on DNA repair mechanisms and therapeutic strategies targeting ATR signaling. -
ATR Inhibitor
ATR-IN-33 is a selective ATR kinase inhibitor that targets the ataxia telangiectasia and Rad3-related protein, involved in the DNA damage response. By inhibiting ATR activity, ATR-IN-33 effectively impairs cellular repair mechanisms, which can lead to enhanced sensitivity to DNA-damaging agents. This compound is valuable for research applications in cancer biology, particularly in studies assessing tumor response to therapy and exploring mechanisms of resistance. -
ATR Inhibitor
Ceralasertib formate is a highly potent and selective inhibitor of ATR (ataxia telangiectasia and Rad3-related protein) with an IC50 value of 1 nM. This compound effectively inhibits cell viability, induces DNA damage, and promotes cellular senescence. Ceralasertib formate demonstrates notable antitumor activity and is valuable for research applications focused on cancer therapeutics and DNA damage response pathways. -
DNA-PK/mTOR Inhibitor
CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively disrupts signaling pathways associated with both mTORC1 and mTORC2. This compound is valuable for research focused on cancer therapeutics and the modulation of DNA damage response mechanisms. -
PI3K Inhibitor
ETP-45658 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) family, exhibiting IC50 values of 22.0 nM for PI3Kα, 39.8 nM for PI3Kδ, 129.0 nM for PI3Kβ, and 717.3 nM for PI3Kγ. Additionally, ETP-45658 demonstrates inhibitory effects on DNA-PK (IC50 = 70.6 nM) and mTOR (IC50 = 152.0 nM). This compound is valuable for cancer research, particularly in exploring the roles of PI3K signaling pathways in tumorigenesis and treatment resistance. -
PI3Kδ Inhibitor
PI3Kδ-IN-27 is a selective inhibitor of PI3Kδ, exhibiting an IC50 value of 355.3 nM. This compound demonstrates notable antiviral activity against SARS-CoV-2, making it a valuable tool for studying viral infections, particularly COVID-19. Researchers can utilize PI3Kδ-IN-27 to explore pathways related to immune response and infection mechanisms. -
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. -
AMPK Pathway Activator
ALKBH1-IN-3 prodrug is a potent inhibitor of the DNA N6-methyladenine demethylase ALKBH1, functioning primarily through modulation of the AMPK signaling pathway. This prodrug significantly enhances the cellular abundance of 6mA, leading to a reduction in the viability of gastric cancer cells. With its strong cellular activity and favorable in vivo metabolic profile, ALKBH1-IN-3 prodrug is a valuable tool for investigating mechanisms underlying gastric cancer and the role of epigenetic modifications in tumor biology. -
AMPKγ3 Activator
PF-07293893 is an AMPKγ3 activator that enhances cellular energy homeostasis. This compound increases glycogen content, improves lipid oxidation, enhances mitochondrial biogenesis, and promotes vascular repair. It is particularly useful in research applications related to heart failure and metabolic disorders. -
AMPK Activator
AMPK Activator 4 is a selective activator of AMP-activated protein kinase (AMPK) that does not inhibit mitochondrial complex I. This compound enhances AMPK activity specifically in muscle tissues, demonstrating a dose-dependent improvement in glucose tolerance in normal mice. Furthermore, it significantly reduces fasting blood glucose levels and ameliorates insulin resistance in db/db diabetic mice, showcasing its potential as an anti-hyperglycemic agent for diabetes research. -
AMPK Activator/GDF15 Inducer
AMPK Activator 12 is a potent activator of AMP-activated protein kinase (AMPK) and serves as an inducer of growth differentiation factor 15 (GDF15). This compound significantly elevates GDF15 protein levels in human hepatic cells, making it a valuable tool for research into metabolic regulation and cellular stress responses. Its ability to modulate these pathways positions AMPK Activator 12 as a crucial reagent for studies on obesity, diabetes, and related metabolic disorders. -
AMPK Activator
AMPK Activator 1 is a potent activator of AMP-activated protein kinase (AMPK), demonstrating an EC50 of less than 0.1 μM. This compound facilitates the phosphorylation of AMPK, thereby enhancing its activity and promoting cellular energy homeostasis. AMPK Activator 1 is valuable for research applications in metabolism, obesity, diabetes, and cancer studies, where modulation of AMPK signaling pathways may provide therapeutic insights. -
AMPK Activator
AMPK-IN-1 is a potent activator of AMP-activated protein kinase (AMPK), specifically targeting the α2β2γ1 isoform with an EC50 of 551 nM. This compound facilitates the phosphorylation of eEF2 through a mechanism that is independent of mTORC1 signaling. AMPK-IN-1 is valuable for research into metabolic regulation and the cellular energy response, offering insights into the therapeutic potential for conditions related to energy imbalances.
