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Catalog No.
Product Name
Application
Product Information
Citations
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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 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 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. -
mTOR Inhibitor/AMPK Activator
AMPK/mTOR modulator-1 is a Ginsenoside derivative functioning as both an mTOR inhibitor and AMPK activator. It activates AMPK signaling with a Kd of 4.759 μM, promoting M1-like tumor-associated macrophage polarization while inhibiting M2-like polarization. This compound enhances glycolysis and demonstrates significant anti-inflammatory activity alongside inhibition of tumor progression. AMPK/mTOR modulator-1 is ideal for research focused on colorectal cancer and related metabolic disorders. -
PI4KB Inhibitor
PI4K-IN-2 is a highly selective inhibitor of phosphatidylinositol 4-kinase β (PI4KB) with an IC50 of 0.015 μM. This compound demonstrates significant inhibitory activity and is particularly relevant for research involving human rhinovirus (HRV). Its potential applications extend to studies focusing on the role of PI4KB in viral replication and related signaling pathways. -
PI4K Inhibitor
KAI-407 is an orally active inhibitor targeting Plasmodium PI4K kinase, effectively disrupting multiple stages of the parasite lifecycle. It demonstrates EC50 values of 81 nM against the blood stages of malignant Plasmodium and 88 nM for liver schizonts of P. yoelii. Additionally, KAI-407 exhibits IC50 values of 0.64 μM and 0.69 μM for liver schizonts and dormant bodies of P. cynomolgi, respectively. This compound is valuable for investigating vivax malaria and assessing potential therapeutic strategies against Plasmodium berghei infections. -
PI4K Inhibitor
BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ), exhibiting an IC50 of 5.7 nM. This compound effectively modulates lipid metabolism and signaling pathways involved in cellular processes. BF738735 is leveraged in research to investigate PI4KIIIβ's role in various diseases, including cancer and viral infections, highlighting its potential for therapeutic development. -
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 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. -
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. -
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. -
ATM Inhibitor
(S)-WSD0628 is a selective ATM inhibitor that effectively inhibits the phosphorylation of ATM in MCF-7 cells, with an IC50 of less than 100 nM. This compound demonstrates radiosensitizing properties, enhancing the efficacy of radiotherapy in cancer treatments. Additionally, (S)-WSD0628 is capable of crossing the blood-brain barrier, making it a valuable tool for research applications in neuro-oncology and other fields where central nervous system exposure is essential. -
ATR Inhibitor
ATR-IN-9 is a selective inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR), with an IC50 value of 10 nM, indicating its high potency. This compound is useful for research applications involving cell cycle regulation, DNA damage response, and cancer therapeutics, offering insights into the role of ATR in cellular processes. Its ability to modulate ATR activity makes it a valuable tool in studies focused on tumor biology and therapeutic resistance. -
ATR Inhibitor
ATR-IN-14 is a potent ATR kinase inhibitor that effectively disrupts ATR signaling pathways by inhibiting CHK1 protein phosphorylation, achieving 98.03% inhibition at 25 nM. With demonstrated anticancer activity in LoVo cells, ATR-IN-14 exhibits an IC50 of 64 nM. This reagent is valuable for researchers investigating DNA damage response mechanisms and therapeutic strategies in cancer treatment. -
ATR Inhibitor
ATR-IN-24 is a potent ATR (Ataxia Telangiectasia and Rad3-related protein) inhibitor. It exhibits significant anticancer activity by interfering with the DNA damage response pathway, thereby enhancing the effects of DNA-damaging agents. This compound is valuable for research applications targeting cancer cell proliferation and sensitivity to chemotherapy, making it an important tool for studies on tumor biology and treatment resistance. -
ATM Inhibitor
ATM Inhibitor-3 is a potent and selective inhibitor of the ataxia-telangiectasia mutated (ATM) kinase, demonstrating an IC50 of 0.71 nM. This compound specifically inhibits the PI3K kinase family, making it relevant for research in cancer biology and DNA damage response pathways. Additionally, ATM Inhibitor-3 exhibits favorable metabolic stability, making it a valuable tool for in vitro and in vivo studies. -
ATR Inhibitor
ATR-IN-6 is a selective inhibitor of ATR (ATM and Rad3-related), a serine/threonine kinase crucial for maintaining genomic stability and facilitating DNA damage repair, belonging to the phosphoinositide 3-kinase-related kinase (PIKK) family. This compound exhibits significant biological activity in the context of ATR-mediated pathways and holds promise for research in proliferative disorders and various cancer types. Its targeted inhibition of ATR can aid in the investigation of therapeutic strategies for diseases associated with DNA damage response dysfunction. -
ATR Inhibitor
ATR-IN-23 is a highly selective inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein) with an IC50 of 1.5 nM. This compound demonstrates significant antiproliferative activity against LoVo cancer cells and induces synthetic lethality in HT-29 cells. ATR-IN-23 is a valuable tool for investigating the mechanisms of DNA damage response (DDR) in cancer research, particularly in the context of DDR-deficient cancer types. -
ATM Inhibitor
ATM Inhibitor-4 is a potent and selective inhibitor of ATM (ataxia-telangiectasia mutated) kinase, exhibiting an IC50 of 0.32 nM. This compound demonstrates enhanced inhibition of the PI3K kinase family and achieves complete inhibition of mTOR at a concentration of 1 μM. Additionally, ATM Inhibitor-4 displays favorable metabolic stability, making it a valuable tool for research applications involving DNA damage response and cell cycle regulation. -
ATM Inhibitor
ATM Inhibitor-6 acts as a selective inhibitor of ATM kinase, interfering with the DNA damage response mechanism. It is valuable for studying cellular processes associated with DNA repair and the proliferation of cancer cells. This reagent is suitable for various cancer research applications, providing insights into the role of ATM in tumorigenesis and therapeutic resistance. -
ATM Inhibitor
ATM Inhibitor-11 is a potent ATM kinase inhibitor with an IC50 value of 0.32 nM. It effectively inhibits the phosphorylation of KAP1, demonstrating an IC50 of 0.97 nM. This compound shows significant pharmacokinetic properties, achieving high exposure levels in the brain, heart, and plasma of ICR mice. Additionally, ATM Inhibitor-11 displays notable anti-tumor activity in the NCI-H441 xenograft mouse model, making it a valuable tool for cancer research and therapeutic development. -
ATM/ATR Inhibitor
ATR-IN-10 is a selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase, exhibiting an IC50 value of 2.978 μM. This compound plays a crucial role in mediating the DNA damage response and is instrumental in studies related to cancer therapeutics, especially in enhancing the efficacy of DNA-damaging agents. ATR-IN-10 is particularly applicable in exploring the interplay between DNA repair mechanisms and cancer cell sensitivity, making it a valuable tool for research in oncology and molecular biology. -
ATR Inhibitor
ATR-IN-32 is a potent inhibitor of the ATR protein kinase, exhibiting oral bioavailability. This compound demonstrates a strong capacity to inhibit the proliferation of MIA PaCa-2 cells and effectively reduces tumor growth in mouse models bearing LOVO and HT-29 xenografts. ATR-IN-32 is applicable in the investigation of ATR-mediated cancer pathways, including those associated with colorectal and pancreatic cancers. -
ATR Inhibitor
ATR-IN-19 is a selective inhibitor of ATR (ATM and Rad3 related) kinase, functioning by disrupting the DNA damage response pathway. This compound has demonstrated potent biological activity in cellular models, making it an invaluable tool for studying the effects of ATR inhibition on cell cycle progression and DNA repair mechanisms. ATR-IN-19 can be employed in cancer research, particularly in investigating therapies that target DNA repair pathways in tumor cells. -
ATM Inhibitor
ATM-IN-1 is a specific inhibitor of Ataxia Telangiectasia Mutated (ATM) protein, which plays a crucial role in cell cycle regulation and the cellular response to DNA damage. By inhibiting ATM, this compound is instrumental in studying the mechanisms of cancer progression and neurological disorders. ATM-IN-1 is valuable for research applications focused on understanding the ATM signaling pathway and its implications in disease models. -
ATR Inhibitor
ATR-IN-15 is a potent inhibitor of ATR kinase, exhibiting an IC50 of 8 nM. This compound demonstrates significant inhibitory effects on human colon tumor cells (LoVo) as well as DNA-PK and PI3K, with IC50 values of 47 nM, 663 nM, and 5131 nM, respectively. ATR-IN-15 is valuable for research into DNA damage response pathways and cancer therapeutics. -
ATR Inhibitor
ATR-IN-21 is a potent inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR), exhibiting an IC50 value of less than 1000 nM. This compound effectively modulates the DNA damage response, making it valuable for research in cancer biology and therapeutic development. ATR-IN-21 can be utilized in studies exploring tumor cell sensitivity to genotoxic agents and the mechanistic pathways of DNA repair. -
ATR Inhibitor
ATR-IN-17 is a potent inhibitor of the Ataxia Telangiectasia and Rad3 related (ATR) kinase. Demonstrating significant anticancer activity, ATR-IN-17 exhibits an IC50 value of 1 nM in LoVo cells, making it a valuable tool for cancer research. This compound is primarily utilized in studies focusing on DNA damage response and cell cycle regulation. -
ATR Inhibitor
ATR-IN-22 is a potent inhibitor of Ataxia Telangiectasia and Rad3-related protein (ATR). This compound effectively reduces the proliferation of MIAPaCa-2 pancreatic cancer cells, exhibiting an IC50 of less than 1 μM. Additionally, ATR-IN-22 demonstrates significant anti-tumor activity in colon cancer, making it a valuable reagent for research into cancer biology and therapeutic development. -
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.
