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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
EGFR Inhibitor
Afatinib N-Oxide is an oxidative degradation product of Afatinib dimaleate, an irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. This compound serves as a valuable tool for characterizing the stability and degradation pathways of Afatinib in chemical research. It may also aid in understanding the mechanistic effects of EGFR inhibition in various biological contexts. -
HPK1 Inhibitor
HPK1-IN-7 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with an IC50 of 2.6 nM, demonstrating excellent selectivity among kinases. It exhibits some selectivity against IRAK4 and GLK, with IC50 values of 59 nM and 140 nM, respectively. This compound has shown significant efficacy in the MC38 syngeneic tumor model, particularly when used in combination with anti-PD1 therapy, highlighting its potential in immuno-oncology research. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
TIE2/STK10/BRK Inhibitor
SB-633825 is a potent ATP-competitive inhibitor targeting TIE2, LOK (STK10), and BRK, with IC50 values of 3.5 nM, 66 nM, and 150 nM, respectively. This compound effectively inhibits cancer cell proliferation and angiogenesis, making it a valuable tool for research on tumor growth and vascular development. Its selective inhibition profile supports studies aimed at understanding the roles of these kinases in cancer biology and therapeutic strategies. -
ErbB-2/EGFR Tyrosine Kinase Inhibitor
GW583340 is an orally bioavailable inhibitor targeting the ErbB-2 and EGFR tyrosine kinases. It demonstrates significant antitumor activity in xenograft models characterized by overexpression of EGFR or ErbB-2, making it a valuable tool for investigating therapeutic strategies. GW583340 is particularly relevant for research focused on head and neck cancer, breast cancer, and gastric cancer. -
ALK Inhibitor
TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development. -
TrkA-NGF Interaction Inhibitor
TrkA/NGF-IN-1 is a potent inhibitor of the interaction between TrkA and nerve growth factor (NGF), with an IC50 of 21 nM as determined by the PathHunter assay. This peptide demonstrates significant analgesic activity in rodent models of incisional pain, making it a valuable tool for research on pain mechanisms and therapeutic interventions targeting the TrkA signaling pathway. -
Trk Kinase Inhibitor
Trk-IN-2 is a potent pan-Trk kinase inhibitor, demonstrating an IC50 of 9 nM for the TrkA enzyme and a cell-based IC50 of 7 nM. This compound exhibits significant pharmacodynamic effects in rat models of inflammatory and neuropathic pain. Trk-IN-2 is valuable for research applications focused on the mechanisms and treatment of inflammatory pain and neuropathic pain conditions. -
EGFR T790M/L858R/ACK1 Inhibitor
EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors. -
Ack1 Inhibitor
Ack1 inhibitor 2 is a selective inhibitor of the Ack1 kinase, demonstrating an IC50 value of 0.46 μM. This compound effectively modulates the Ack1 signaling pathway, which plays a critical role in various cellular processes, including cell proliferation and survival. Ack1 inhibitor 2 is primarily utilized in research applications focused on cancer biology and molecular signaling studies. -
ALK Inhibitor
XMU-MP-5 is a selective inhibitor of anaplastic lymphoma kinase (ALK), demonstrating potent inhibitory activity against ALK-mutated Ba/F3 cells with IC50 values ranging from 4 to 50 nM. This compound induces apoptosis specifically in EML4-ALK Ba/F3 cells and has shown notable antitumor efficacy in murine models. XMU-MP-5 serves as a valuable tool in cancer research, particularly in studies focused on ALK-driven malignancies. -
ALK Inhibitor
Ceritinib mesylate is a selective ALK tyrosine kinase inhibitor that functions through ATP-competitive mechanisms, exhibiting an IC50 of 200 pM. In addition to its activity against ALK, Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D, with IC50 values of 8 nM, 7 nM, and 23 nM, respectively. This compound demonstrates significant antitumor potency, making it a valuable tool for research in cancer biology and targeted therapies. -
DDR Inhibitor
7rh is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 13.1 nM, and also demonstrates moderate inhibitory activity against DDR2 with an IC50 of 203 nM. This compound serves as a valuable tool for the study of receptor signaling and cellular processes associated with DDRs. Additionally, 7rh incorporates an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it suitable for applications in click chemistry. -
DDR1 DDR2 FLT1 Inhibitor
TPKI-39 is an inhibitor of DDR1, DDR2, and FLT1, demonstrating a human DDR1 IC50 of 380 nM and human DDR2 IC50 of 120 nM. It effectively inhibits enzymatic activity and autophosphorylation of DDR1 and DDR2, as well as FLT1 enzymatic activity, with an IC50 of 65 nM. This compound is useful for studies focused on the modulation of receptor tyrosine kinases and collagen-mediated signaling pathways. -
TIE2 Inhibitor
BAY-826 is a selective and potent inhibitor of the TIE2 receptor, exhibiting a binding affinity (Kd) of 1.6 nM. This compound plays a significant role in studying angiogenesis and vascular biology by modulating TIE2 signaling pathways. Its application in research encompasses tumor microenvironment studies, vascular disorder investigations, and potential therapeutic strategies targeting vascular-related diseases. -
DDR1/2 Inhibitor
VU6015929 is a potent and selective dual inhibitor of discoidin domain receptors 1 and 2 (DDR1/2), exhibiting IC50 values of 4.67 nM and 7.39 nM, respectively. This compound effectively inhibits collagen-induced activation of DDR1 and reduces collagen-IV production, making it a valuable tool for research on fibrosis and extracellular matrix remodeling. VU6015929 is suitable for studying the roles of DDR1/2 in various pathological processes and therapeutic interventions. -
Discoidin Domain Receptor Inhibitor
DDR1-IN-4 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), effectively blocking its autophosphorylation with an IC50 of 29 nM. This compound exhibits significantly lower activity against DDR2, with an IC50 of 1.9 μM. DDR1-IN-4 is utilized in research applications focusing on cell signaling, extracellular matrix interactions, and cancer biology, providing valuable insights into the role of DDR1 in various pathological conditions. -
DDR2 Inhibitor
DDR2-IN-1 is a potent inhibitor of the Discoidin Domain Receptor 2 (DDR2) with an IC50 of 26 nM. This compound plays a significant role in research related to osteoarthritis by modulating collagen signaling pathways and potentially influencing cartilage degradation and repair. Its application in studying DDR2-mediated processes makes it a valuable tool for investigating therapeutic strategies in bone and joint diseases. -
DDR1 Inhibitor
DDR1-IN-6 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), exhibiting an IC50 of 9.72 nM. This compound effectively inhibits auto-phosphorylation at the Y513 site of DDR1b, also with an IC50 of 9.7 nM, demonstrating significant anti-cancer activity. Additionally, DDR1-IN-6 serves as a click chemistry reagent due to its alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, facilitating diverse research applications in chemical biology and drug discovery. -
Discoidin Domain Receptor Inhibitor
DDR Inhibitor is a highly selective inhibitor of the discoidin domain receptors (DDRs), specifically demonstrating an IC50 of 3.3 nM for DDR2. Additionally, it exhibits a significant inhibitory effect on DDR1, with 53% inhibition at a concentration of 1.5 nM. This compound is valuable for investigating the role of DDRs in cellular processes and may have applications in cancer research and fibrosis studies. -
DDR1/DDR2 Inhibitor
DDR1/2 inhibitor-2 is a selective inhibitor of the DDR1 and DDR2 receptor tyrosine kinases, demonstrating IC50 values of less than 100 nM. This compound is primarily utilized in research related to cancer and fibrotic diseases, providing insights into the role of these receptors in tumor progression and fibrosis. Its potent inhibitory effects make it a valuable tool for studying DDR signaling pathways and their contributions to disease mechanisms. -
DDR1 Inhibitor
DDR1-IN-5 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), demonstrating an IC50 of 7.36 nM. It effectively inhibits the auto-phosphorylation of DDR1b at Y513, with an IC50 of 4.1 nM. DDR1-IN-5 exhibits anti-cancer activity, making it a valuable tool for cancer research. Additionally, this compound features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition for further biochemical applications. -
Discoidin Domain Receptor Inhibitor
DDR1-IN-9 is a selective inhibitor of the Discoidin Domain Receptor 1 (DDR1), known for its significant suppression of kinase activity, with a Kd value of 4.7 nM and an IC50 value of 9.4 nM. Demonstrating reduced activity against a broad panel of 400 nonmutated kinases, DDR1-IN-9 exhibits a favorable specificity profile. This compound also possesses beneficial pharmacokinetic properties and has displayed potential therapeutic effects in experimental models of pulmonary fibrosis, making it a valuable tool for researching fibrotic diseases and DDR1-related signaling pathways. -
DDR1 Inhibitor
DDR1-IN-10 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1). It exhibits significant potential in the modulation of DDR1-mediated signaling pathways, making it a valuable tool in cancer research. DDR1-IN-10 is particularly useful for studying various malignancies, including pancreatic cancer, non-small cell lung cancer, and gastric carcinoma, where DDR1 plays a critical role in tumor progression and metastasis. -
DDR1/2 Inhibitor
DDR1/2 IN-4 is a selective dual inhibitor targeting DDR1 and DDR2 kinases, demonstrating a pKi of 8.6 for DDR1 and 8.2 for DDR2. This compound effectively inhibits the kinase activities of both DDR1 and DDR2, leading to a reduction in the release of MCP-1. DDR1/2 IN-4 is suitable for research applications focused on idiopathic pulmonary fibrosis and related cellular mechanisms. -
DDR1 Inhibitor
DDR1-IN-12 is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 0.126 μM. This compound effectively blocks receptor tyrosine kinase autophosphorylation, thereby inhibiting downstream signaling pathways, including the suppression of TGF-β1-induced fibroblast activation. DDR1-IN-12 demonstrates significant potential in research applications related to tumor cell migration and the progression of pulmonary fibrosis, making it particularly relevant for studies involving lung cancer, including lung adenocarcinoma. -
DDR1/2 Inhibitor
DDR1-IN-8 is a potent dual inhibitor of DDR1 and DDR2, demonstrating IC50 values of 0.045 μM and 0.126 μM, respectively. This compound exhibits significant anti-tumor activity, making it a valuable tool for studies related to cancer research. DDR1-IN-8 can be utilized to explore the role of DDR signaling in tumor progression and therapeutics targeting the DDR pathway. -
DDR1/2 Inhibitor
DDR1/2 inhibitor-3 is a selective inhibitor of discoidin domain receptor 1 and 2 (DDR1/2), exhibiting IC50 values of 9.4 nM and 20.4 nM, respectively. This compound is primarily utilized in anti-inflammatory research, targeting the DDR pathways involved in cellular responses to inflammation. Its potent inhibitory effects make it a valuable tool for elucidating the role of DDR receptors in various biological processes. -
EphB2 Inhibitor
ALW-II-49-7 is a selective inhibitor of the EphB2 kinase, exhibiting an EC50 value of 40 nM in cellular assays. It is designed to effectively disrupt EphB2 signaling pathways, which are implicated in various biological processes including cell adhesion and migration. This reagent is valuable for research applications focusing on cancer biology, neurodevelopment, and the modulation of angiogenesis. -
EphA3 Inhibitor
AWL-II-38.3 is a selective inhibitor of the ephrin-A receptor (EphA3) kinase. This compound demonstrates potent inhibitory activity specifically targeting EphA3 while displaying minimal effects on Src-family kinases and b-raf. Its specificity makes AWL-II-38.3 valuable for research applications involving EphA3-mediated signaling pathways and related cellular processes. -
EphB3 Inhibitor
LDN-211904 oxalate is a potent and reversible inhibitor of EphB3, exhibiting an IC50 of 79 nM. This compound demonstrates favorable metabolic stability in mouse liver microsomes, making it suitable for in vitro studies. LDN-211904 oxalate is particularly relevant for research involving STAT3-activated colorectal cancer stemness and may help overcome Cetuximab resistance in colorectal cancer. -
Eph Inhibitor
Eph Inhibitor 1 is a potent inhibitor of Eph receptors, targeting the Eph family of receptor tyrosine kinases. It has demonstrated significant biological activity in modulating cellular signaling pathways involved in neural development and synaptic plasticity. This compound holds promise for research applications related to neurological disorders, facilitating insights into therapeutic strategies for conditions linked to Eph receptor dysregulation. -
EPHA2 Inhibitor
EphA2 antagonist 1 is an ephrin type-A receptor 2 (EPHA2) inhibitor designed to modulate the signaling pathways associated with this receptor. It exhibits significant biological activity in disrupting EPHA2-mediated processes, which may have implications in cancer research and metastasis studies. This compound serves as a valuable tool for investigating the role of EPHA2 in various cellular contexts and therapeutic applications. -
EphB4, VEGFR-2 and PDGFR-β Inhibitor
JI-101 hydrochloride is an orally active inhibitor targeting EphB4, VEGFR-2, and PDGFR-β, effectively modulating angiogenesis signaling pathways associated with tumor vasculature. This compound demonstrates significant anti-cancer activity, inhibiting multiple stages of tumor angiogenesis and showing efficacy against various cancer cell lines and xenografts. With rapid oral absorption and extensive tissue distribution, preferential uptake occurs in the lungs, while elimination primarily occurs via feces. JI-101 hydrochloride can be utilized in research studies focused on ovarian cancer and other solid tumors, providing valuable insights into angiogenesis and cancer treatment mechanisms. -
EphB4 Inhibitor
EphB4-IN-2 is a potent tyrosine kinase inhibitor targeting EphB4, with an IC50 value of 1.6 nM in human assays. This compound demonstrates selective inhibition against kinases containing threonine gatekeeper residues, offering a high degree of ligand efficiency. Its application is valuable in research focusing on EphB4-related signaling pathways and associated therapeutic interventions. -
EphB3 Inhibitor
LDN-211904 is a potent and reversible inhibitor of EphB3, with an IC50 of 79 nM, making it a valuable tool for studying EphB3-mediated signaling pathways. It demonstrates good metabolic stability in mouse liver microsomes, indicating its potential for in vivo applications. In research contexts, LDN-211904 may synergize with cetuximab to effectively inhibit STAT3 activation and address colorectal cancer stemness, as well as resistance mechanisms associated with cetuximab treatment. -
ITK Inhibitor
Soquelitinib is a selective covalent inhibitor of interleukin-2-inducible kinase (ITK). It exhibits significant anti-inflammatory activity across multiple models of T cell-mediated inflammatory diseases, including asthma, pulmonary fibrosis, systemic sclerosis, psoriasis, and acute graft-versus-host disease. By inhibiting Th2 cytokine production, Soquelitinib enhances the infiltration of CD8+ T cells into tumors, promoting improved T effector function and potential therapeutic benefits in oncology and immunology research. -
ITK Inhibitor
GNE-9822 is a potent and selective inhibitor of ITK (Interleukin-2-inducible T-cell kinase) with a Ki value of 0.7 nM and an EC50 value of 354.5 nM. This compound demonstrates favorable ADME properties, making it suitable for in vivo studies. GNE-9822 is primarily utilized in research on asthma and other related immunological conditions, providing insights into the modulation of T-cell signaling pathways.
