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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR Inhibitor
EAI001 is a potent allosteric inhibitor of the mutant epidermal growth factor receptor (EGFR), specifically targeting the EGFRL858R/T790M variant with an IC50 of 24 nM. This compound demonstrates selective inhibition of aberrant EGFR signaling, making it valuable for investigating its role in cancer biology and therapeutic resistance. EAI001 serves as a critical tool for research aimed at understanding and developing treatments for EGFR-mutated tumors. -
EGFR/ErbB Inhibitor
EGFR/ErbB-2-IN-2 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and ErbB family of receptor tyrosine kinases. It exhibits IC50 values of 0.017 μM for EGFR, 0.08 μM for ErbB-2, and 1.91 μM for ErbB-4, highlighting its selectivity and efficacy. This compound is valuable for research applications focused on cancer biology, particularly in the study of signaling pathways and mechanisms associated with EGFR and ErbB receptor activation. -
EGFR Inhibitor
Rociletinib hydrobromide is a selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), particularly effective against the T790M mutation. It demonstrates a Ki value of 21.5 nM for the EGFRL858R/T790M variant, while maintaining a Ki of 303.3 nM for wild-type EGFR. This compound is relevant for research applications aimed at understanding and developing targeted therapies for EGFR-mutant cancers. -
EGFR Inhibitor
Tyrphostin AG 112 is a selective inhibitor of epidermal growth factor receptor (EGFR) phosphorylation. This compound has been shown to interfere with EGFR signaling pathways, resulting in the inhibition of cell proliferation and survival in various cancer cell lines. Tyrphostin AG 112 is utilized in research applications aimed at understanding EGFR-mediated processes and developing targeted therapies for EGFR-associated tumors. -
HER2/EGFR Inhibitor
Neratinib maleate is an orally available, irreversible inhibitor targeting HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively. This compound demonstrates significant anti-tumor activity and is utilized in research for its applications in cancer therapy, particularly in tumors exhibiting overexpression of HER2. Its selective inhibition profile makes it a valuable tool for studies exploring resistance mechanisms and therapeutic efficacy in targeted cancer treatment. -
EGFR-HER2 Inhibitor
Sevabertinib is a potent and reversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values below 0.5 nM for both wild-type HER2 and various mutant forms, including HER2 A775insYVMA, as well as wild-type EGFR and EGFR D770_N771insSVD. This compound demonstrates significant anticancer activity, particularly against lung cancer, making it a valuable tool for research in targeted cancer therapies and signaling pathway studies. -
EGFR/ErbB2 Inhibitor
PD 174265 is a highly selective, reversible inhibitor of the EGFR and ErbB2 tyrosine kinases, demonstrating an IC50 of 0.45 nM. This compound effectively inhibits receptor autophosphorylation and the downstream ERK signaling pathway, leading to significant antitumor activity and reduced toxicity in in vivo models. Additionally, PD 174265 facilitates the differentiation of oligodendrocyte precursor cells, promoting the expression of myelin proteins such as CNP, PLP, and MBP, and enhancing neurite branching. With no inhibitory effect on other kinases like insulin and PDGF receptors, PD 174265 is a vital tool for researching human epidermoid carcinoma treatment and myelin repair mechanisms in multiple sclerosis. -
EGFR/ERBB2 Inhibitor
HKI-357 is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM for EGFR and 33 nM for ERBB2. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, leading to the inhibition of downstream signaling pathways, including AKT and MAPK phosphorylation. HKI-357 is valuable for research into cancer therapies that target these critical signaling pathways. -
IGF-1R Inhibitor
AZ7550 Mesylate is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting an inhibitory concentration (IC50) of 1.6 μM. It is utilized in research to study the role of IGF-1R in cellular signaling pathways, cancer proliferation, and resistance mechanisms. This compound serves as a valuable tool for understanding IGF-1R-related diseases and may aid in the development of targeted therapies. -
FGFR1 Inhibitor
PD-161570 is a potent ATP-competitive inhibitor of the human fibroblast growth factor receptor 1 (FGFR1) with an IC50 of 39.9 nM and a Ki of 42 nM. It also demonstrates inhibitory effects on platelet-derived growth factor receptor (PDGFR), epidermal growth factor receptor (EGFR), and c-Src tyrosine kinases, with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. Additionally, PD-161570 effectively inhibits PDGF-stimulated autophosphorylation and FGFR phosphorylation, with IC50s of 450 nM and 622 nM, respectively. This compound is relevant in studies of bone morphogenetic proteins (BMPs) and TGF-β signaling pathways. -
EGFR Inhibitor
EGFR-IN-70 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 23.6 nM and 307.5 nM for EGFR-LR/TM/CS and EGFR-WT, respectively. This compound demonstrates significant anti-proliferative effects and effectively suppresses EGFR phosphorylation. EGFR-IN-70 is a valuable tool for cancer research, particularly in studies focusing on EGFR-related signaling pathways and therapeutic interventions. -
EGFR Kinase Inhibitor
PF-06672131 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, targeting the ATP-binding pocket through its alkynylated afatinib derivative structure. This small molecule probe displays reactivity to cysteine and is valuable for activity-based protein profiling studies. Its ability to effectively inhibit EGFR makes it a useful tool in cancer research, particularly in exploring therapeutic strategies for EGFR-driven malignancies. -
EGFR Tyrosine Kinase Inhibitor
Mavelertinib is a highly selective, orally bioavailable irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent inhibitory activity with IC50 values of 5 nM, 4 nM, 12 nM, and 3 nM against Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. This compound is primarily utilized in research related to non-small-cell lung cancer (NSCLC). -
EGFR Inhibitor
Oritinib is an irreversible third-generation inhibitor targeting the epidermal growth factor receptor (EGFR). It effectively overcomes T790M-mediated resistance in non-small cell lung cancer by selectively inhibiting various mutant forms of EGFR, including EGFRWT, EGFRL858R, EGFRL861Q, and both EGFRL858R/T790M and EGFRd746-750 mutations, with low IC50 values ranging from 0.1 to 18 nM. This compound is valuable for research applications focusing on cancer therapeutics and mechanisms of drug resistance. -
Src Inhibitor
β-Hydroxyisovalerylshikonin is a natural product derived from Lithospermum erythrorhizon, functioning as a potent Src inhibitor. It exhibits significant inhibitory activity against protein tyrosine kinases, with IC50 values of 0.7 μM for EGFR and 1 μM for the v-Src receptor. This compound demonstrates broad anticancer activity, particularly inducing cell death in various tumor cell lines, most notably in NCI-H522 and DMS114 cells, making it a valuable tool for cancer research applications. -
EGFR/FLT3/Abl Inhibitor
Ruserontinib is an orally active multikinase inhibitor targeting EGFR, FLT3, and Abl. With an IC50 of 55 nM for human FLT3, it demonstrates significant antitumor activity. This compound is primarily utilized in cancer research, particularly for studying the effects of inhibiting key kinases involved in tumor progression and survival. -
EGFR Inhibitor
EGFR-IN-95 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting del19/T790M/C797S and L858R/T790M/C797S mutations. This 2,4-diaminonicotinamide derivative exhibits strong biological activity, making it valuable for research on various EGFR-driven malignancies. Its use is particularly relevant in studies focused on developing targeted therapies for resistant forms of lung cancer and other EGFR-related conditions. -
Mutant-Selective EGFR Inhibitor
Osimertinib-d6 is a deuterium-labeled derivative of osimertinib, a covalent and orally active inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants. With an IC50 of 12 nM against the L858R mutation and 1 nM against L858R/T790M, osimertinib-d6 demonstrates potent efficacy in overcoming T790M-mediated resistance. This compound is valuable for research applications focused on targeted lung cancer therapies and the mechanisms of drug resistance in EGFR-driven tumors. -
EGFR Inhibitor
JCN037 is a non-covalent inhibitor targeting the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity with IC50 values of 2.49 nM for EGFR, 3.95 nM for p-wtEGFR, and 4.48 nM for pEGFRvIII, indicating its effectiveness in inhibiting various EGFR forms. This compound is particularly useful for research applications in cancer biology, especially in studies focused on EGFR signaling pathways and therapeutic resistance mechanisms. Its ability to penetrate the blood-brain barrier further extends its potential in neuro-oncological research. -
EGFR Inhibitor
(E/Z)-AG490 is a racemic mixture of the (E)-AG490 and (Z)-AG490 isomers, functioning as a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates inhibitory activity against other targets, including Stat-3 and the Janus kinases JAK2/3, making it valuable for research in signal transduction and cancer biology. Its ability to modulate key pathways involved in cell proliferation and survival positions (E/Z)-AG490 as an important tool for studying therapeutic strategies in oncology. -
EGFR Inhibitor
EGFR kinase inhibitor 3 is a bivalent ATP-allosteric inhibitor targeting the epidermal growth factor receptor (EGFR) kinase. It demonstrates potent inhibitory activity, with IC50 values of less than 10 nM for wild-type EGFR and as low as 0.059 nM for the L858R/T790M/C797S triple mutant. This compound is particularly useful for studies involving EGFR-mediated signaling pathways and can aid in the development of targeted therapies for EGFR-driven cancers. -
Alflutinib Metabolite/EGFR Inhibitor
AST5902 trimesylate is the primary metabolite of Alflutinib, functioning as an EGFR inhibitor. This compound demonstrates significant antineoplastic activity, making it a valuable reagent for cancer research. Its utility in exploring EGFR-related signaling pathways and therapeutic mechanisms can aid in the development of targeted cancer treatments. -
EGFR-TKI Inhibitor
PKI-166 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating potent activity with an IC50 of 0.7 nM. It exhibits oral bioavailability and is utilized in research focused on cancer therapies that target aberrant EGFR signaling pathways. PKI-166 serves as a valuable tool for investigating the role of EGFR in tumorigenesis and evaluating the efficacy of EGFR-targeted treatments in various cancer models. -
EGFR/ErbB2 Inhibitor
Selatinib is a reversible and orally bioavailable dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2, demonstrating IC50 values of 13 nM and 22.5 nM, respectively. This compound exhibits significant anticancer activity, making it a valuable tool for research in targeted cancer therapies and studies focused on EGFR and ErbB2 signaling pathways. -
EGFR Mutants Inhibitor
Pruvonertinib is an orally active inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), including the T790M mutation and exon 20 insertions. This compound has demonstrated significant antitumor activity, leading to tumor regression in patient-derived xenograft models driven by EGFR exon 20 insertions. Pruvonertinib is a valuable reagent for research in cancer biology, particularly in studies focused on resistant mutations in lung cancer therapeutics. -
EGFR Inhibitor
Simotinib is a selective, orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 value of 19.9 nM. This compound exhibits significant antineoplastic activity, making it a valuable tool for cancer research. Simotinib is primarily utilized in studies investigating the molecular mechanisms of EGFR signaling and the development of targeted therapies for EGFR-dependent tumors. -
EGFR Inhibitor
BBT-176 is a potent oral inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant inhibitory activity against various EGFR C797S mutant cell lines, making it a valuable tool for investigating resistance mechanisms in cancer therapy. This compound is widely utilized in cancer research to explore alternative treatment strategies targeting EGFR-related pathways. -
EGFR Inhibitor
EGFR-IN-197 is a potent inhibitor of the Epidermal Growth Factor Receptor (EGFR), displaying IC50 values of 19.5 nM and 12.0 nM against the EGFRL858R/T790M and EGFRL858R/T790M/C797S mutations, respectively. This compound effectively arrests the cell cycle in the G2/M phase, inhibiting proliferation, colony formation, and migration of NCI-H1975 cells. Additionally, EGFR-IN-197 disrupts anti-apoptotic signaling pathways, induces DNA damage, and activates pro-apoptotic pathways, thereby triggering apoptosis. Its properties make it a valuable reagent for research focused on non-small cell lung cancer (NSCLC). -
TrxR/EGFR Inhibitor
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer. -
ErbB-2/EGFR Inhibitor
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling. -
CSF1R/c-Kit Inhibitor
Pexidartinib hydrochloride is a potent, orally active inhibitor of the colony stimulating factor 1 receptor (CSF1R) and c-Kit, demonstrating ATP-competitive activity with IC50 values of 20 nM and 10 nM, respectively. This compound exhibits selective inhibition, with 10- to 100-fold potency over other related kinases. Pexidartinib hydrochloride promotes apoptosis in affected cells and exhibits significant anti-cancer properties, making it a valuable tool for research in oncology and immunology. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-2 is a dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Dihydrofolate Reductase (DHFR), exhibiting IC50 values of 0.623 μM and 9.085 μM, respectively. This compound demonstrates significant cytotoxic activity against various cancer cell lines, including C26, HepG2, and MCF7, with IC50 values ranging from 3.59 to 8.38 μM. VEGFR-2/DHFR-IN-2 is pertinent for research applications focused on cancer therapeutics and targeted inhibition of tumor angiogenesis. -
VEGFR-2/DHFR Inhibitor
VEGFR-2/DHFR-IN-1 is a dual inhibitor of VEGFR-2 and dihydrofolate reductase (DHFR), exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. This compound demonstrates significant antibacterial activity against various strains, including Escherichia coli and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, VEGFR-2/DHFR-IN-1 shows potent cytotoxic effects on cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM. This reagent is applicable for research exploring cancer therapeutics and microbial resistance. -
TRAF6-p62 Inhibitor
TRAF6 peptide is a selective inhibitor of the TRAF6-p62 interaction. It effectively disrupts the ubiquitination of TrkA in NGF-dependent signaling pathways. This peptide demonstrates significant potential for research in neurological disorders, including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, epilepsy, and stroke. -
TIE-2 Inhibitor
TP-S1-68 is a potent TIE-2 inhibitor with an IC50 of 3.65 μM. This compound demonstrates significant antibacterial activity against a range of bacterial and fungal pathogens. TP-S1-68 serves as a valuable starting point for the development of novel TIE-2 inhibitors and is applicable in research focused on solid tumors, as well as bacterial and fungal infections. -
DDR/p38 Inhibitor
SR-302 is a selective DDR/p38 inhibitor that exhibits potent biological activity with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. This compound is valuable for investigating fibrotic disorders, including renal and pulmonary fibrosis, atherosclerosis, and various types of cancer. SR-302 serves as a key tool for elucidating the roles of DDR and p38 signaling pathways in disease progression and therapeutic intervention. -
IRAK4 Inhibitor
UR241-2 is a selective inhibitor of IRAK4, targeting the IL-1–induced IRAK1/4 signaling pathway. It effectively suppresses NF-κB activation and the phosphorylation of p65 and p38, contributing to a reduction in leukemia stem cell clonogenicity. UR241-2 also serves as a valuable ligand for developing PROTAC degraders targeting IRAK4, making it a suitable tool for research in acute myeloid leukemia. -
CDK2 Inhibitor
TrkA Inhibitor is a selective CDK2 inhibitor, demonstrating an IC50 of 0.69 μM against CDK1. This compound is particularly valuable in research focused on chemotherapy-induced alopecia, allowing for the investigation of mechanisms involved in hair follicle cycling and potential therapeutic interventions. Its specificity for CDK2 makes it a useful tool in examining cell cycle regulation and associated pathways in various biological contexts. -
EphB4/Src Kinase Inhibitor
AZ12672857 is a potent inhibitor of EphB4 and Src kinases, demonstrating an IC50 of 1.3 nM for EphB4. This compound significantly inhibits the proliferation of c-Src transfected 3T3 cells with an IC50 of 2 nM and autophosphorylation of EphB4 in CHO-K1 cells with an IC50 of 9 nM. AZ12672857 can be utilized in studies investigating signaling pathways related to cancer and cell growth regulation. -
IRAK4 Inhibitor
Zabedosertib is a selective inhibitor of IRAK4, a protein kinase integral to the signaling pathways of innate immune responses triggered by Toll-like receptors. With an IC50 of 3.55 nM, Zabedosertib demonstrates significant immunomodulatory effects, specifically exhibiting anti-inflammatory activity against IL-1β, lipopolysaccharide (LPS), and Imiquimod-induced inflammation. This compound is suitable for research applications focused on exploring innate immunity and inflammation modulation. -
IRAK1 Inhibitor
JH-X-119-01 is a selective inhibitor of interleukin-1 receptor-associated kinases 1 (IRAK1) that demonstrates significant potential in immunological research. With an IC50 of 9 nM, JH-X-119-01 effectively inhibits IRAK1 activity without affecting IRAK4 at concentrations up to 10 μM. This compound has been shown to mitigate LPS-induced sepsis in animal models, making it a valuable tool for studies focused on inflammation and sepsis-related pathways. -
IRAK-4 Inhibitor
Edecesertib is a selective and potent inhibitor of the interleukin-1 receptor-associated kinase 4 (IRAK-4). It exhibits significant anti-inflammatory activity, making it valuable in the study of inflammatory diseases. Edecesertib is applicable in research focused on rheumatoid arthritis (RA) and lupus erythematosus (LE), contributing to the understanding of therapeutic targets in these conditions. -
IRAK1 Inhibitor
JH-X-119-01 hydrochloride is a selective inhibitor of interleukin-1 receptor-associated kinase 1 (IRAK1), a key player in inflammatory signaling pathways. This compound demonstrates significant potential in reducing LPS-induced sepsis in murine models, indicating its utility in studying inflammatory disorders. Researchers can leverage JH-X-119-01 hydrochloride to explore IRAK1's role in immune responses and develop targeted therapies for sepsis and related conditions. -
IRAK4 Inhibitor
IRAK4-IN-21 is a potent and selective inhibitor of IRAK4, exhibiting IC50 values of 5 nM for IRAK4 and 56 nM for TAK1. This orally active compound effectively inhibits interleukin-23 (IL-23) production with an IC50 of 0.17 μM. IRAK4-IN-21 is valuable for research applications in autoimmune diseases, particularly in the context of plaque psoriasis and psoriatic arthritis. -
IRAK Inhibitor
IRAK4-IN-6 is a selective inhibitor of IRAK4, demonstrating an IC50 of 4 nM. It effectively targets the MyD88 L265P mutant variant associated with diffuse large B cell lymphoma, making it a valuable tool for research in oncology and immune signaling pathways. Its oral efficacy supports in vivo studies, facilitating investigations into IRAK4's role in tumorigenesis and potential therapeutic interventions. -
IRAK4 Inhibitor
IRAK4-IN-22 is a selective IRAK4 inhibitor with potent activity, exhibiting IC50 values of 3 nM for IRAK4 and 17 nM for TAK1. This compound effectively inhibits IL-23 production with an IC50 of 0.10 µM, making it a valuable tool for research into autoimmune conditions such as plaque psoriasis and psoriatic arthritis. Its oral bioavailability enhances its suitability for in vivo studies, facilitating investigations into the therapeutic potential of targeting IRAK4 in inflammatory diseases. -
IRAK4 Inhibitor
BIO-7488 is a selective IRAK4 inhibitor with a potent IC50 of 0.5 nM, designed to cross the blood-brain barrier effectively. This compound inhibits the production of pro-inflammatory cytokines, including IL-1β, TNFα, and IL-6, displaying significant anti-inflammatory properties in both LPS-induced and distal hypoxic-middle cerebral artery occlusion ischemic stroke models. BIO-7488 is a valuable reagent for researching neuroinflammatory disorders, particularly in the context of ischemic stroke. -
IRAK4 Inhibitor
IRAK4-IN-20 is a potent inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), showcasing an IC50 of 3.55 nM. This compound is indicated for research into inflammatory conditions, particularly acute respiratory distress syndrome (ARDS). Its mechanism of action makes it a valuable tool for studying IRAK4's role in immune signaling pathways and related therapeutic interventions. -
IRAK4 Inhibitor
GLPG2534 is a selective inhibitor of IRAK4, exhibiting IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4 respectively. This compound effectively modulates inflammatory signaling pathways involved in immune responses. GLPG2534 is suitable for research aimed at understanding and developing treatments for inflammatory skin diseases. -
IRAK4 Inhibitor
IRAK4-IN-14 is a potent, selective inhibitor of IRAK4, demonstrating an IC50 of 0.003 µM. This orally active compound exhibits favorable pharmacokinetic properties in both rat and mouse models. IRAK4-IN-14 has shown synergy in vitro against MyD88/CD79 double mutant ABC-DLBCL when used in combination with Acalabrutinib, making it a valuable tool for research in oncology and inflammation pathways.
