Catalog No.
Product Name
Application
Product Information
Citations
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ALK5 Inhibitor
PF-03671148 is a selective inhibitor of ALK5, a receptor kinase involved in TGFβ signaling. This compound effectively attenuates TGFβ-induced fibrotic gene expression in fibroblasts, making it a promising candidate for research on fibrosis and related conditions. PF-03671148 may hold significant potential for therapeutic applications aimed at preventing dermal scarring and modulating fibrotic responses in various tissues. -
ALK2 Inhibitor
LDN-193688 is a selective inhibitor of ALK2, exhibiting IC₅₀ values of 104, 18, 235, 1530, and 1080 nM against ALK1, ALK2, ALK3, ALK4, and ALK5, respectively. This compound effectively inhibits bone morphogenetic protein 4 (BMP4)-induced phosphorylation of SMAD1/5/8, with an IC₅₀ of 2.6 μM. LDN-193688 is utilized in research focused on the BMP signaling pathway and its role in various biological processes, including development and disease. -
ALK/ROS1 Inhibitor
ALK/ROS1-IN-4 is a selective dual inhibitor targeting the anaplastic lymphoma kinase (ALK) and ROS1 kinases. This compound exhibits potent inhibitory activity against both kinases, making it a valuable tool for studying signaling pathways involved in certain cancers. ALK/ROS1-IN-4 is primarily used in research applications focused on cancer biology and therapeutic development for ALK- and ROS1-positive malignancies. -
ALK Inhibitor
CEP-28122 mesylate hydrochloride is a selective, orally active inhibitor of the anaplastic lymphoma kinase (ALK) with a reported IC50 of 1.9 nM. Exhibiting significant antitumor activity, it is effective in experimental models of ALK-positive malignancies, including anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma. Its favorable pharmacodynamic and pharmacokinetic properties make it a valuable tool for research into ALK-driven cancers. -
ALK inhibitor
Alectinib analog is a selective inhibitor of Anaplastic Lymphoma Kinase (ALK), specifically designed to overcome resistance via gating mutations. This compound shows low micromolar IC50 values, indicating potent antiproliferative and cytotoxic effects against cancer cells. Its efficacy is linked to enhanced stability and the release of active components. Additionally, Alectinib analog has been demonstrated to inhibit vascular septal dimensions in an in vivo zebrafish model, highlighting its potential for therapeutic applications in cancer research. -
c-FMS(CSF-IR)/c-Kitdual Inhibitor
Vimseltinib is a selective dual inhibitor of c-FMS (CSF-IR) and c-Kit, demonstrating IC50 values of less than 0.01 μM and 0.1-1 μM, respectively. This compound exhibits robust biological activity, making it a valuable tool for investigating signaling pathways involved in hematopoiesis and various pathologies such as cancer and inflammatory diseases. The oral bioavailability of Vimseltinib enhances its potential for in vivo studies and therapeutic applications. -
c-kit Inhibitor
Bezuclastinib is a highly selective inhibitor of the c-kit tyrosine kinase, demonstrating potent activity against the KIT D816V mutation. This compound is valuable for researching nonadvanced systemic mastocytosis (NonAdvSM) and provides insight into the underlying mechanisms of this condition. Its oral bioavailability makes it a convenient option for in vivo studies targeting c-kit dysregulation. -
CSF1R Inhibitor
Pimicotinib is a selective and orally active inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R), with an IC50 value of 19.48 nM as determined by the inhibition of ADP production. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research applications aimed at understanding tumor microenvironment interactions and immune modulation. Researchers can utilize Pimicotinib to explore CSF1R-mediated signaling in cancer biology and potential therapeutic strategies. -
Tyrosine Kinase Inhibitor
Elenestinib is a selective orally active tyrosine kinase inhibitor, demonstrating a potent inhibitory effect on the KIT D816V mutant with an IC50 value of 6 nM. Its mechanism of action is primarily focused on inhibiting aberrant signaling pathways associated with systemic mastocytosis. Due to its limited ability to cross the blood-brain barrier, Elenestinib is particularly applicable in the investigation of hematologic disorders related to mast cell proliferation and activity. -
c-Kit Inhibitor
c-Kit-IN-5 is a potent c-Kit inhibitor, demonstrating IC50 values of 22 nM in kinase assays and 16 nM in cellular assays. This compound exhibits over 200-fold selectivity for c-Kit compared to other kinases, such as KDR, p38, Lck, and Src. Due to its favorable pharmacokinetic properties, c-Kit-IN-5 is well-suited for research applications exploring c-Kit-related signaling pathways and their implications in various diseases, including cancer. -
c-Kit/PDGFR Inhibitor
Labuxtinib is a potent dual inhibitor of c-Kit and PDGFR, effectively blocking cell proliferation driven by c-Kit or PDGFR signaling pathways. This compound is suitable for research applications targeting mast cell-associated diseases, respiratory conditions, inflammatory disorders, fibrosis, and metabolic diseases. Its dual mechanism of action makes Labuxtinib a valuable tool for investigating the molecular underpinnings of these diseases and potential therapeutic strategies. -
VEGFR/PDGFα/c-Kit Inhibitor
Telatinib mesylate is a potent, orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit, exhibiting IC50 values of 6 nM, 4 nM, 15 nM, and 1 nM respectively. This compound effectively impedes angiogenesis and tumor cell proliferation, making it a valuable tool in cancer research. Its selective targeting of key signaling pathways has potential applications in studying tumor microenvironments and in developing therapeutic strategies for various malignancies. -
Tyrosine Kinase Inhibitor
Elenestinib phosphate is an orally active tyrosine kinase inhibitor that selectively targets the KIT D816V mutation, exhibiting an IC50 of 0.2 nM. This compound's targeted inhibition is particularly relevant for studying systemic mastocytosis, as it provides insights into the role of mutated KIT in this condition. Notably, elenestinib phosphate has limited capacity to penetrate the blood-brain barrier, making it suitable for investigating its effects in peripheral tissues. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis. -
c-Kit Inhibitor
c-Kit-IN-7 is a potent c-Kit inhibitor that demonstrates an IC50 of ≤10 nM. It effectively inhibits cell proliferation in GIST430 and BaF3 mutant cell lines, with IC50 values of ≤100 nM. This compound is crucial for research focused on cancers driven by c-KIT kinase mutations, providing valuable insights into therapeutic strategies targeting this pathway. -
CSF1R Inhibitor
Pimicotinib hydrochloride is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R), demonstrating an IC50 value of 19.48 nM in inhibiting ADP production. This compound exhibits notable anti-tumor activity, making it a valuable tool for research in cancer biology and immunotherapy. Its specificity for CSF1R provides insights into the modulation of macrophage activity in the tumor microenvironment. -
FMS/KIT Inhibitor
PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, exhibiting IC50 values of 28 nM and 16 nM, respectively. This compound demonstrates high selectivity for FMS and KIT over a broad spectrum of 400 kinases at a concentration of 1 μM, with minimal activity against FLT3 and KDR (IC50s of 91 nM and 130 nM, respectively). PLX647 dihydrochloride is valuable for research applications focused on hematopoietic and oncogenic signaling pathways. -
c-kit Inhibitor
c-Kit-IN-14 is a selective inhibitor of the c-Kit kinase, effectively blocking its phosphorylation with an IC50 of 0.4 nM for pKIT. It demonstrates potent activity against Exon 11 c-Kit mutations, also with an IC50 of 0.4 nM. This compound is primarily utilized in research related to mast cell-mediated disorders, including urticaria, providing insights into therapeutic strategies targeting c-Kit signaling pathways. -
c-kit Inhibitor
c-Kit-IN-13 is a highly selective c-kit kinase inhibitor that effectively blocks the autophosphorylation of wild-type c-kit, demonstrating an IC50 of 0.3 nM for pKIT and 0.9 nM for Exon 11 KIT. This compound is particularly useful in researching mast cell-mediated conditions, including urticaria, providing insights into the role of c-kit in these pathologies. Its potent inhibitory activity makes it a valuable tool for studies focused on targeted therapies in hematological cancers and related disorders. -
c-KIT/PDGFR/RET Inhibitor
KBP-7018 hydrochloride is a selective inhibitor of tyrosine kinases, specifically targeting c-KIT, PDGFR, and RET. It exhibits significant inhibitory potency, with IC50 values of 10 nM, 7.6 nM, and 25 nM, respectively. This compound is utilized in research focused on idiopathic pulmonary fibrosis, facilitating investigations into pathways associated with this condition. -
Kit Inhibitor
APcK110 is a potent inhibitor of the Kit receptor tyrosine kinase, with applications in the study of acute myeloid leukemia (AML). This compound has been shown to induce apoptosis in AML cells, offering valuable insights into therapeutic strategies for targeting this malignancy. Researchers can utilize APcK110 to explore mechanisms of resistance, cell signaling pathways, and potential combination therapies in AML treatment. -
c-Kit Inhibitor
KI-328 is a selective inhibitor of the c-Kit kinase, specifically designed to target various mutant forms associated with acute myeloid leukemia (AML). It demonstrates effective inhibition of both wild-type and certain mutant KIT-expressing cell lines, although it shows diminished activity against the D816V-KIT variant. Comparative analyses with other potent KIT inhibitors indicate varying degrees of efficacy across different mutant forms, highlighting the necessity for targeted assessments in clinical applications. KI-328 provides a valuable tool for research focused on the biological mechanisms of KIT mutations and their implications in leukemia therapies. -
c-Kit Inhibitor
c-Kit-IN-11 is a selective inhibitor of c-Kit, exhibiting an IC50 of 76 nM in Mo7e cells. This compound is valuable in research related to inflammatory conditions such as asthma, as well as in the study of malignant cancers. Its targeted inhibition of c-Kit makes it a useful tool for investigating the underlying mechanisms of these diseases and potential therapeutic strategies. -
FLuc Inhibitor
GW694590A is an inhibitor targeting firefly luciferase (Fluc) that enhances the stability of the MYC protein, subsequently increasing its endogenous levels. This compound also inhibits receptor tyrosine kinases, demonstrating significant reductions in DDR2, KIT, and PDGFRα activity at 1 μM. GW694590A serves as a versatile protein kinase inhibitor, influencing both ATP-dependent and -independent luciferase systems, making it valuable for studies in cellular signaling and gene expression regulation. -
c-Kit Inhibitor
c-Kit-IN-8 is a selective inhibitor of the c-Kit kinase, demonstrating high efficacy with an IC50 greater than 1 μM for uKIT kinase. It effectively reduces the proliferation of cancer cells, including GIST430 and BaF3 cell lines, with an IC50 of over 0.1 μM. This compound is valuable for research in cancer biology, particularly in studies focusing on c-Kit-related signaling pathways and therapeutic resistance in oncogenesis. -
c-Kit Inhibitor
c-Kit-IN-10 is a selective inhibitor of the c-Kit receptor tyrosine kinase, which plays a critical role in hematopoiesis, cell signaling, and tumorigenesis. This compound demonstrates potent anti-proliferative activity against c-Kit-dependent cancers and has potential applications in the study of inflammatory conditions such as asthma. Researchers may utilize c-Kit-IN-10 to investigate its therapeutic effect on disease models characterized by aberrant c-Kit signaling. -
VEGFR Inhibitor
Tafetinib analogue 1 is a selective inhibitor of the vascular endothelial growth factor receptor (VEGFR). This compound exhibits potent anti-angiogenic activity, making it a valuable tool for investigating the role of VEGFR in tumor growth and metastasis. Tafetinib analogue 1 is applicable in cancer research, particularly in studies focusing on therapeutic strategies targeting the VEGF signaling pathway. -
IRAK4 PROTAC Degrader
PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis. -
SRC Stimulator
(E/Z)-MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator that enhances SRC activity in cancer cells. This leads to the overstimulation of reactive oxygen species (ROS) production, resulting in cell stress and apoptosis through a mechanism known as paraptosis. (E/Z)-MCB-613 serves as a cytotoxic agent with significant implications for cancer research, particularly in studies focusing on targeted cancer therapies and mechanisms of cell death. -
c-MET ADC
Zevontabart (MYTX-011 Antibody) is a pH-dependent antibody-drug conjugate (ADC) targeting c-MET. It interferes with the trafficking of c-MET, leading to reduced receptor recycling and enhanced endocytosis in c-MET-expressing cells. Zevontabart demonstrates significant cytotoxicity against solid tumor cells and exhibits anti-tumor efficacy in non-small cell lung cancer xenograft models. This reagent is valuable for research in non-small cell lung cancer and related studies. -
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. -
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. -
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. -
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. -
Bioactive Peptide
IRAK-4 Peptide substrate (IRAK-1 residues 360-380) is a bioactive peptide specifically designed to serve as a substrate for Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4). This peptide facilitates the study of IRAK-4's role in signal transduction pathways associated with inflammatory responses. It is suitable for applications in cellular signaling research, particularly in the context of immune system studies and cytokine signaling. -
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. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-3 is a PROTAC-based ligand designed to target and induce the degradation of interleukin-1 receptor-associated kinase 4 (IRAK4) via the von Hippel-Lindau (VHL) E3 ubiquitin ligase. This compound effectively modulates the inflammatory response by selectively degrading IRAK4, making it a valuable tool for exploring therapeutic strategies in inflammatory diseases and immune signaling pathways. Its application in research can provide insights into IRAK4's role in various pathologies, including cancer and autoimmune disorders. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-8 is a targeted protein degradation compound designed to selectively degrade IRAK4, demonstrating an IC50 of 15.5 nM. This reagent effectively induces IRAK4 degradation in THP-1 cells with a DC50 of 1.8 nM. Additionally, PROTAC IRAK4 Degrader-8 inhibits L-6 production in human whole blood and LPS-induced human peripheral blood mononuclear cells, exhibiting IC50 values of 246 nM and 2.2 nM, respectively. This compound is a valuable tool for studying the role of IRAK4 in immune responses and offers potential applications in inflammatory and autoimmune research. -
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. -
IRAK4 Inhibitor
PF-06426779 is a potent and selective inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK4), displaying an IC50 of 0.3 nM. This compound effectively modulates inflammatory signaling pathways and is useful in the study of diseases related to dysregulated immune responses. Researchers can leverage PF-06426779 in experimental settings exploring the roles of IRAK4 in cellular processes and potential therapeutic interventions in inflammation-driven disorders.
