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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Tubulin Polymerization/Akt Pathway Inhibitor
KS-99 is an inhibitor that targets both tubulin polymerization and the Akt signaling pathway. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis in various cancer cell types. KS-99 is suitable for research applications involving colorectal cancer, breast cancer, lung epithelial cancer, and melanoma. -
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. -
PI4KIIIα Inhibitor
GSK-A1 is a selective inhibitor of type III phosphatidylinositol 4-kinase PI4KIIIα, exhibiting a pIC50 of 8.5-9.8. It effectively inhibits the resynthesis of PtdIns(4,5)P2 with an IC50 of approximately 3 nM, leading to a potent decrease in PtdIns(4)P levels without significantly affecting PtdIns(4,5)P2. GSK-A1 serves as a valuable tool in research aimed at understanding its potential role in anti-hepatitis C virus (HCV) applications. -
PI4KIIIβ Inhibitor
MI 14 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ), demonstrating an IC50 of 54 nM for this target, while exhibiting limited activity against PI4KIIIα and PI4KIIα with IC50s greater than 100 μM. This compound displays notable antiviral efficacy against hepatitis C virus (HCV) genotype 1b, Coxsackievirus B3 (CVB3), human rhinovirus (HRV), and HCV genotype 2a. MI 14 serves as a valuable tool for research focused on viral pathogenesis and therapeutic interventions targeting lipid kinase signaling pathways. -
PI4KIIIα/HCV Inhibitor
AL-9 is a potent inhibitor of phosphatidylinositol 4-kinase III alpha (PI4KIIIα) with an IC50 of 0.57 μM. It effectively disrupts hepatitis C virus (HCV) replication, making it a valuable tool for studying viral pathogenesis and potential antiviral strategies. Its selective targeting of PI4KIIIα highlights its relevance in research applications focused on HCV infection and related therapeutic developments. -
mTOR Inhibitor
Aschantin is a bisepoxylignan that acts as a potent mTOR kinase inhibitor. This compound demonstrates significant biological activities, including antiplasmodial effects, calcium channel antagonism, and the inhibition of platelet activating factor. Additionally, Aschantin serves as an inhibitor of Cytochrome P450 and UGT enzymes, making it a valuable tool for chemoprevention research and various biochemical studies. -
mTORC1 Inhibitor
Sulindac sulfone is an mTORC1 pathway inhibitor and an active metabolite of Sulindac. It has been shown to effectively inhibit the growth of colon cancer cells and induce cell cycle arrest, making it a valuable tool in cancer research. This compound is primarily utilized to study the role of mTORC1 in tumorigenesis and to explore potential therapeutic strategies against colorectal cancer. -
PI3Kα Inhibitor
VVD-442 is a selective inhibitor of PI3Kα that covalently binds to cysteine 242 within the RAS-binding domain of the PI3K p110α subunit. This binding induces conformational changes that disrupt the interaction between PI3K p110α and RAS proteins, effectively blocking RAS-mediated activation of PI3K. VVD-442 is applicable in research focusing on RAS-mutant cancers and HER2-overexpressing tumors, providing valuable insights into therapeutic strategies targeting these pathways. -
PI3Kδ Inhibitor
LAS195319 is a potent and orally active inhibitor of PI3Kδ, exhibiting an IC50 of 0.5 nM. This compound demonstrates high selectivity against a wide array of proteins, lipid kinases, and GPCRs. LAS195319 effectively inhibits the infiltration of neutrophils and eosinophils, making it a valuable tool for research into respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD). -
PI3Kγ Inhibitor
SH-273 is a potent dual-function compound that acts as a selective inhibitor of PI3Kγ with an IC50 of 7 nM while also stimulating STING function with an EC50 of 100 nM. This unique profile makes SH-273 a valuable tool for investigating signaling pathways involved in pancreatic cancer. Researchers can utilize SH-273 to explore the therapeutic potential of targeting PI3Kγ and enhancing STING-mediated immune responses in cancer models. -
COX-2/PI3K Inhibitor
COX-2/PI3K-IN-2 is a potent inhibitor targeting both COX-2 and PI3K pathways, exhibiting an IC50 value of 2.78 nM for PI3K and a Ki value of 3.02 nM for COX-2. This compound demonstrates significant anti-inflammatory and anti-cancer activities, making it valuable for research in oncology and inflammatory disease studies. Its dual-target mechanism provides insights into the therapeutic potential of modulating these critical pathways. -
PI3Kδ Inhibitor
IHMT-PI3Kδ-372 is a highly selective inhibitor of PI3Kδ, exhibiting an IC50 of 14 nM. This compound demonstrates significant selectivity over other class I PI3Ks, with 56 to 83-fold differences, as well as over various protein kinases. IHMT-PI3Kδ-372 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), enabling investigations into therapeutic strategies targeting this pathway. -
PI3K Inhibitor
Isopsoralidin is a phosphatidylinositol 3-kinase (PI3K) inhibitor that demonstrates potentially hepatotoxic properties and exhibits inhibitory activity on CYP2D6. This compound plays a significant role in research focused on cell signaling pathways related to cancer and metabolic disorders. Its unique mechanism of action makes it a valuable tool for studying PI3K-related biological processes and evaluating therapeutic approaches involving PI3K modulation. -
mTORC1/glucose transporter Inhibitor
NV-5440 is an inhibitor of the mechanistic target of rapamycin complex 1 (mTORC1) and glucose transporters GLUT-1, GLUT-2, GLUT-3, and GLUT-4. This compound effectively inhibits glucose uptake in cells, providing valuable insights into glucose metabolism and its regulation. NV-5440 is useful for research applications involving cancer metabolism, diabetes, and other metabolic disorders where mTORC1 signaling and glucose transport play significant roles. -
mTORC1/S6K1 Inhibitor
Coronarin A is a natural compound that functions as an inhibitor of mTORC1 and S6K1, enhancing IRS1 activity. This compound exhibits anti-inflammatory properties and is relevant for research into type 2 diabetes mellitus. Its modulation of key signaling pathways makes Coronarin A a valuable tool for studying metabolic disorders and inflammation-related conditions. -
PI3K/mTOR Inhibitor
NVP-BBD130 is a potent dual inhibitor of PI3K and mTOR, functioning through ATP-competitive mechanisms. This compound demonstrates significant stability and provides effective oral bioavailability. Additionally, NVP-BBD130 serves as a click chemistry reagent due to its alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its versatility makes it suitable for various research applications in cancer therapy and biochemical signaling pathways. -
PI3K Inhibitor
Zandelisib is a selective, orally active, non-covalent inhibitor of PI3Kδ. It effectively inhibits AKT phosphorylation and suppresses downstream signaling pathways, making it a valuable tool in cancer research. Zandelisib is particularly relevant for studying malignancies such as relapsed or refractory B-cell lymphoma, providing insights into tumor behavior and therapeutic response. -
NUAK1 Inhibitor
NUAK1-IN-3 is a selective inhibitor of NUAK1 with a high potency, exhibiting an IC50 of 0.49 nM. It also demonstrates inhibitory activity against NUAK2 and JAK3 with IC50 values of 265 nM and 225 nM, respectively. This compound disrupts the NUAK1-MYPT1 signaling pathway, leading to reduced MYPT1 phosphorylation and inhibition of proliferation, migration, and invasion in triple-negative breast cancer cells. Additionally, NUAK1-IN-3 counteracts TGF-β1-induced epithelial-mesenchymal transition effects by modulating critical markers such as Snail, N-cadherin, and E-cadherin. It holds potential for exploring therapeutic strategies for triple-negative breast cancer. -
SGK1/GSK3β Inhibitor
SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders. -
mTORC2 Inhibitor
JR-AB2-011 is a selective inhibitor of the mTORC2 complex, exhibiting an IC50 value of 0.36 μM. This compound disrupts the association between Rictor and mTOR (Ki: 0.19 μM), leading to reduced phosphorylation of Akt and decreased MMP2 activity. Consequently, JR-AB2-011 inhibits the migratory and invasive capabilities of tumor cells while also triggering non-apoptotic cell death. It serves as a valuable tool for research into cancer treatment and the regulation of cellular signaling pathways. -
mTORC1 Inhibitor
RMC-5552 is a potent and selective inhibitor of the mTORC1 pathway. It effectively inhibits the phosphorylation of S6K and 4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. RMC-5552 demonstrates significantly lower inhibition of AKT (IC50 of 19 nM), conferring a selectivity ratio for mTORC1 over mTORC2 of nearly 40-fold. This compound exhibits anti-cancer activity, making it a valuable tool for cancer research and therapeutic development targeting mTOR signaling.
