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Catalog No.
Product Name
Application
Product Information
Citations
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ITK Inhibitor
ITK inhibitor 6 is a highly selective inhibitor of ITK with an IC50 of 4 nM. This compound also demonstrates weaker activity against BTK, JAK3, EGFR, and LCK, with IC50 values of 133 nM, 320 nM, 2360 nM, and 155 nM, respectively. ITK inhibitor 6 effectively inhibits the phosphorylation of PLCĪ³1 and ERK1/2 pathways and exhibits significant antiproliferative activity. It is a valuable tool for research applications focused on lymphocyte signaling and cancer biology. -
ITK Inhibitor
ITK-IN-6 is a potent and selective inhibitor of Interleukin-2-inducible T-cell kinase (ITK), with a Kd of 387 nM. It directly targets the ITK kinase domain, effectively blocking the release of pro-inflammatory cytokines and modulating the activation and differentiation of Th2 and Th17 cells. This compound demonstrates significant potential in asthma research by reducing inflammatory cell infiltration, mucus production, and IgE levels, thereby mitigating airway inflammation and improving asthma progression. -
ITK Inhibitor
ITK inhibitor 5 is a selective inhibitor targeting the interleukin-2-inducible T-cell kinase (ITK) with an IC50 of 5.6 nM. Demonstrating low activity against Bruton's tyrosine kinase (BTK) with an IC50 of 25 nM, this compound is useful in studying T-cell signaling pathways and immune responses. It serves as an effective tool in research aimed at understanding the role of ITK in various hematological disorders and inflammatory diseases. -
Itk Inhibitor
ITK/TRKA-IN-1 is a selective inhibitor targeting IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA), exhibiting an IC50 of 1.0 nM for ITK and achieving 96% inhibition of TRKA. This compound is valuable for investigating the roles of ITK and TRKA in immune responses and neurobiology. Its dual inhibitory action positions it as a significant tool for research in cancer immunotherapy and neurodegenerative disease studies, enabling the exploration of signaling pathways associated with these kinases. -
AXL Inhibitor
Axl-IN-20 is a selective AXL inhibitor with a potent IC50 of 5 nM. This orally active compound demonstrates significant anti-tumor activity, particularly against hematological malignancies. It is a valuable tool for research applications aimed at understanding AXL signaling pathways and developing targeted cancer therapies. -
TAM Receptor Inhibitor
TAM-IN-1 is a potent macrocyclic inhibitor targeting TAM receptors Axl and Mer, displaying binding affinities with Kis of 130 pM and <50 pM, respectively. This compound demonstrates significant biological activity in modulating pathways associated with tumor progression and immune evasion. TAM-IN-1 is applicable in research focused on cancer therapeutics and the study of receptor-mediated signaling in the tumor microenvironment. -
TYRO3 Inhibitor
UNC9426 is a highly selective inhibitor of TYRO3, exhibiting an IC50 of 2.1 nM and demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. This compound effectively reduces platelet aggregation without prolonging bleeding time, and it inhibits TYRO3-mediated processes in both tumor cells and macrophages. With a favorable safety profile, UNC9426 is an invaluable tool for investigating TYRO3-dependent phenotypes, including applications in non-small cell lung cancer (NSCLC) research. -
AXL Inhibitor
Ligritinib is an AXL receptor tyrosine kinase inhibitor that displays oral bioavailability. It effectively inhibits AXL kinase activity, disrupting downstream signaling pathways associated with cancer progression. Ligritinib is particularly relevant in cancer research, and it is often investigated in combination with chemotherapy for the treatment of non-small cell lung cancer (NSCLC). -
MER/AXL Inhibitor
BPR5K230 is a dual inhibitor targeting the receptor tyrosine kinases MER and AXL, exhibiting IC50 values of 4.1 nM and 9.2 nM, respectively. This compound effectively inhibits the proliferation of Ba/F3-MER cells, with an IC50 of 5 nM. In preclinical models, BPR5K230 demonstrates anti-inflammatory and antitumor activities against various cancer cell lines, including 4T1, MDA-MB-231, MC38, and Hepa1-6, as well as favorable pharmacokinetic properties in mice. These attributes make BPR5K230 a valuable tool for research into cancer biology and targeted therapies. -
TAM Receptor Inhibitor
AZ14145845 is a selective inhibitor targeting the TAM receptor kinases Mer and Axl, classified as a type I1/2 dual kinase inhibitor. This compound demonstrates notable in vivo efficacy, making it a valuable tool for research in cancer biology and therapeutic resistance mechanisms. Its selective inhibition of the TAM receptors contributes to the modulation of immune responses and potential enhancement of antitumor activity, serving as a significant asset in studies focused on cancer treatment and immunotherapy. -
Axl Inhibitor
TL4830031 is a potent Axl inhibitor, exhibiting an IC50 value of 26 nM. This compound effectively disrupts Axl phosphorylation, leading to inhibition of cell invasion and migration. TL4830031 is an ideal reagent for cancer research applications, providing valuable insights into tumor biology and potential therapeutic interventions targeting the Axl pathway. -
AXL Inhibitor
Axl-IN-6 is a potent AXL inhibitor that demonstrates significant anti-tumor activity. This orally active compound effectively inhibits tumor growth in the MV-4-11 subcutaneous xenograft model, showcasing its potential for cancer research applications. Axl-IN-6 is well tolerated, making it a suitable candidate for evaluating AXL targeting in therapeutic studies. -
MerTK Inhibitor
MerTK-IN-3 is a selective MerTK inhibitor, demonstrating an IC50 of 21.5 nM for MerTK while maintaining a significantly higher IC50 of 991.3 nM for Tyro3. This compound is suitable for research applications focused on colon cancer, enabling studies into MerTK's role in tumor progression and potential therapeutic interventions. Its oral bioavailability further enhances its utility in preclinical studies. -
AXL Inhibitor
Axl-IN-9 is a potent inhibitor of AXL, exhibiting an IC50 of 26 nM. This compound demonstrates excellent transmembrane and pharmacokinetic properties, making it suitable for in vivo studies. Axl-IN-9 is intended for research applications in proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, cancer, and other related mammalian diseases. -
AXL Inhibitor
Axl-IN-11 is a potent AXL inhibitor that targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in the modulation of cell proliferation and migration, making it useful in the study of various proliferative and autoimmune diseases, as well as in cancer research. Additionally, Axl-IN-11 can be applied in the investigation of allergic, inflammatory, and viral infectious diseases, as well as transplant rejection mechanisms in mammals. -
AXL Inhibitor
Axl-IN-4 is an AXL kinase inhibitor that demonstrates an IC50 of 28.8 Ī¼M. This compound specifically targets the AXL receptor tyrosine kinase, which is implicated in multiple cancer pathways and immune responses. Axl-IN-4 is useful for research applications aiming to elucidate the roles of AXL in tumor progression and to explore potential therapeutic strategies against AXL-driven malignancies. -
AXL inhibitor
Axl-IN-17 is a selective AXL inhibitor that demonstrates potent inhibitory activity with an IC50 value of 3.2 nM. This compound exhibits significant antitumor efficacy, making it a valuable tool for research in cancer biology. Axl-IN-17 is suitable for studies focusing on AXL-mediated signaling pathways and their implications in tumor progression and metastasis. -
AXL Inhibitor
Axl-IN-10 is a potent AXL inhibitor with an IC50 of 5 nM, effectively targeting the AXL receptor. This compound exhibits favorable transmembrane and pharmacokinetic properties, enhancing its utility in biological research. Axl-IN-10 is applicable in the study of various proliferative diseases, autoimmune disorders, allergic reactions, inflammatory conditions, transplant rejection, and cancer, making it a valuable tool for researchers exploring these complex pathologies in mammals. -
MerTK Inhibitor
UNC3133 is a selective and orally bioavailable inhibitor of the Mer tyrosine kinase (MerTK), demonstrating an IC50 of 8.1 nM. This compound exhibits preferential inhibition of the TAM receptor family, particularly with approximately sevenfold selectivity for Axl and tenfold selectivity for Tyro3, while also showing comparable activity against Flt3. UNC3133 is applicable in research focused on anti-tumor and anti-infection mechanisms, providing insights into therapeutic strategies targeting these pathways. -
AXL Inhibitor
Axl-IN-12 is a potent AXL inhibitor that selectively targets the AXL receptor tyrosine kinase. It exhibits significant biological activity in regulating cell proliferation and modulating immune responses. Axl-IN-12 is suitable for research applications related to proliferative diseases, autoimmune disorders, allergic responses, inflammation, transplant rejection, various malignancies, and viral infections in mammalian systems. -
Axl Inhibitor
AXL-IN-15 is a highly potent inhibitor of the Axl receptor tyrosine kinase, exhibiting Ki and IC50 values of less than 1 nM. This compound is valuable for research focused on cancer biology, particularly in studies investigating Axl's role in tumor progression and metastasis. AXL-IN-15 can aid in elucidating the molecular mechanisms underlying Axl-mediated signaling pathways and their implications in various malignancies. -
AXL Inhibitor
Axl-IN-7 is a potent inhibitor of the AXL receptor tyrosine kinase. This compound demonstrates significant activity in targeting AXL-mediated signaling pathways, making it valuable for investigating AXL-related diseases, including various cancers such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors. Additionally, Axl-IN-7 has potential applications in research focused on renal diseases, immune system disorders, and cardiovascular conditions. -
MerTK/Axl Inhibitor
MerTK/Axl-IN-1 is a highly selective dual inhibitor targeting MerTK and Axl receptors, demonstrating potent inhibitory activity with IC50 values of 4.2 nM and 8.8 nM in Ba/F3 cells, and 0.2 nM and 0.9 nM in HTRF assays. This compound effectively inhibits phosphorylated MerTK (pMerTK) in vivo, indicating its utility in biological research. With a prolonged half-life and favorable oral bioavailability, MerTK/Axl-IN-1 is suitable for studies in cancer biology and therapeutic development aimed at disruptions in MerTK and Axl signaling pathways. -
AXL Inhibitor
Axl-IN-19 is a selective inhibitor of AXL, a membrane-bound receptor tyrosine kinase, exhibiting an IC50 of 5.3 nM and a cellular KD of 6.8 nM. This compound demonstrates favorable pharmacokinetic properties in rats, characterized by low clearance and moderate bioavailability. Axl-IN-19 is primarily utilized in cancer research to explore the role of AXL signaling in tumor progression and metastasis. -
TAM Receptor Inhibitor
MerTK-IN-1 is an inhibitor of the MerTK receptor, a critical target in the regulation of tumor-associated macrophages (TAMs). This compound demonstrates the ability to effectively bind to MerTK in vivo, providing valuable insight into immune modulation in tumor microenvironments. MerTK-IN-1 is suitable for research applications focused on cancer immunotherapy and the role of macrophages in tumor progression. -
Gas6/Axl Inhibitor
Anticancer agent 109 is a Gas6/Axl inhibitor that demonstrates significant anti-cancer activity. This compound effectively downregulates the expression of Gas6 and Axl, which in turn reduces the activation of p-PI3K and p-AKT in cancer cells. Anticancer agent 109 induces G1 phase cell cycle arrest and promotes apoptosis, leading to substantial inhibition of tumor growth in nude mouse models. This reagent is suitable for research focused on cancer biology and therapeutic development targeting the Gas6/Axl signaling pathway. -
TYRO3/MERTK Inhibitor
UNC9435 is a dual inhibitor of TYRO3 and MERTK, exhibiting IC50 values of 3.7 nM and 1.1 nM, respectively. This compound has been shown to significantly reduce colony formation in non-small cell lung cancer cultures, indicating its potential as a therapeutic agent in cancer research. UNC9435 may also serve as a useful tool for studying the role of TYRO3 and MERTK in various biological processes and disease mechanisms. -
AXL Inhibitor
Axl-IN-3 is a selective inhibitor of the AXL kinase, demonstrating potent activity with an IC50 of 41.5 nM. This compound has shown minimal inhibition of other kinases, making it an ideal choice for studies focused on AXL-mediated signaling pathways. Axl-IN-3 is suitable for research applications involving cancer biology, immune modulation, and therapeutic resistance studies. -
MERTK/AXL Inhibitor
UNC8969 is a dual inhibitor targeting MERTK and AXL, exhibiting IC50 values of 1.1 Ā± 0.8 nM for MERTK and 5.3 Ā± 2.7 nM for AXL. With a half-life (T1/2) of 7.3 hours following intravenous administration at 5 mg/kg in mice, UNC8969 demonstrates significant biological activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the roles of MERTK and AXL in tumor progression and immune modulation. -
AXL Inhibitor
AXL-IN-14 is a highly potent, orally bioavailable inhibitor of AXL, exhibiting an impressive IC50 value of 0.8 nM. This compound effectively disrupts Gas6/AXL-mediated cell migration and invasion while reducing the expression levels of phospho-AXL and phospho-AKT proteins. AXL-IN-14 demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer therapeutics and metastasis studies. -
AXL Inhibitor
Axl-IN-5 is a selective inhibitor of AXL, exhibiting an IC50 of 283 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology. Axl-IN-5 can be utilized to study the role of AXL signaling in tumor progression and to investigate potential therapeutic strategies targeting the AXL pathway in various malignancies. -
MET/AXL Inhibitor
(Z)-S49076 hydrochloride is a potent inhibitor of MET and AXL, effectively disrupting their downstream signaling pathways. This compound demonstrates significant biological activity by inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. Additionally, (Z)-S49076 hydrochloride addresses resistance mechanisms associated with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in Erlotinib-resistant cell lines. It is a valuable tool for research in non-small cell lung cancer (NSCLC). -
AXL Inhibitor
Denfivontinib hydrochloride is an AXL inhibitor that exerts synergistic antitumor effects when used in combination with the PD-1 inhibitor Pembrolizumab. This compound enhances the NOD-like receptor pathway, facilitating the formation of the NLRP3 inflammasome. Its unique mechanism of action makes it a valuable tool for cancer research, particularly in studying immune modulation and tumor progression. -
AXL Inhibitor
ER-851 is a selective inhibitor of AXL with an IC50 of 100 nM, demonstrating potent oral bioactivity. It has been shown to exhibit antitumor effects, making it a valuable compound for research in cancer biology and therapeutic development. Its selectivity and efficacy position ER-851 as a critical tool for studying AXL's role in tumor progression and metastasis. -
Tie2 Inhibitor
6-Hydroxy-2,2ā²,4,4ā²-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, exhibiting an IC50 value of 2.1 Ī¼M. This compound interacts with the ATP binding site of Tie2, effectively inhibiting its kinase activity and thereby blocking tumor angiogenesis. It is a valuable tool for research focused on vascular biology and cancer therapeutics. -
Tie2 Inhibitor
Tie2 kinase inhibitor 2 is a selective inhibitor of the Tie2 kinase with an IC50 value of 1 Ī¼M. It effectively inhibits endothelial cell tube formation, making it a valuable tool for investigating Tie2-mediated angiogenic disorders. This compound is suitable for research focused on angiogenesis and related therapeutic applications. -
Tie-2 Kinase Inhibitor
Tie2 Kinase Inhibitor 3 is a potent inhibitor of the Tie-2 kinase, exhibiting an IC50 value of 30 nM. By competing with the ATP binding site of Tie-2, this compound effectively inhibits phosphorylation and signaling pathways associated with Tie-2, thereby influencing the stability and maturation of blood vessels. Its mechanisms provide valuable insights into tumor angiogenesis, making Tie2 kinase inhibitor 3 a significant tool for research focused on restricting tumor growth and modulating angiogenic processes. -
Tie2 Inhibitor
BSF-466895 is a potent Tie2 inhibitor with an IC50 value of 5 nM, demonstrating significant inhibition of Tie1 as well. This compound is valuable for research applications focused on vascular biology and angiogenesis, as well as exploring the therapeutic potential in disorders related to angiogenic dysregulation. BSF-466895 serves as a useful tool for elucidating the role of the Tie2 signaling pathway in various biological contexts. -
ALK4/5/7 Inhibitor
A 83-01 sodium is a selective inhibitor of the transforming growth factor-beta (TGF-Ī²) type I receptors ALK4, ALK5, and ALK7. With IC50 values of 12 nM, 45 nM, and 7.5 nM, it effectively blocks transcriptional activity induced by these kinases. This compound is valuable for research applications focused on TGF-Ī² signaling pathways and regulation of cellular processes such as proliferation, differentiation, and epithelial-mesenchymal transition. -
ALK2 Inhibitor
M4K-2009 is a potent inhibitor of ALK2, exhibiting an IC50 value of 13 nM, and is capable of penetrating the blood-brain barrier. In addition to its primary activity against ALK2, M4K-2009 demonstrates efficacy against the hERG potassium channel. This compound is valuable for research in the areas of bone morphogenetic protein signaling and related therapeutic applications. -
SRC-3 Inhibitor
SI-2 hydrochloride is a potent inhibitor of SRC-3, a transcription co-regulator involved in various signaling pathways. This compound displays favorable pharmacokinetic properties and reduced toxicity, making it suitable for in vivo studies. SI-2 hydrochloride is valuable for research related to cancer biology, endocrine signaling, and other conditions where SRC-3 plays a critical role. -
ITK/TRK Inhibitor
PF-07245303 is an ITK/TRK inhibitor that effectively reduces the production of pro-inflammatory cytokines such as IL-4 and IFNĪ³. This compound inhibits the phosphorylation of PLCĪ³1 and disrupts nerve growth factor-induced basophil activation and TRKA phosphorylation. Additionally, PF-07245303 demonstrates a reduction in oxazolone-induced ear swelling in mouse models, making it a valuable tool for research into atopic dermatitis and related inflammatory conditions. -
VEGFR2 Inhibitor
VEGFR2-IN-84 is a potent VEGFR2 inhibitor that operates as a multi-targeted tyrosine kinase inhibitor utilizing a naphthalene ring scaffold. It exhibits sub-nanomolar affinity for VEGFR2 and effectively inhibits other kinases, including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 disrupts the phosphorylation of VEGFR2, leading to significant reduction in endothelial cell proliferation, migration, and tumor angiogenesis. This compound demonstrates broad antiproliferative activity against various solid tumors, such as liver, lung, and renal cancers, while exhibiting low toxicity to normal cells. VEGFR2-IN-84 is suitable for research applications focused on malignant tumors. -
EGFR Inhibitor
ZW-49 is a potent orally active pan-EGFR inhibitor, demonstrating IC50 values ranging from 0.03 to 1.5 nM. This compound selectively targets various EGFR mutations while sparing wild-type EGFR and other familial targets, effectively blocking the ATP-binding pocket and a conserved hydrophobic subpocket without causing steric conflicts with PACC mutation P loops. ZW-49 exhibits significant anti-proliferative activity by inhibiting cancer cell proliferation, inducing G0/G1 phase cell-cycle arrest, and promoting apoptosis, making it a valuable reagent for cancer research, particularly in non-small cell lung cancer models. -
EGFR Inhibitor
Rinumafusp alfa is a human monoclonal antibody that specifically inhibits the epidermal growth factor receptor (EGFR) by targeting ERBB3/HER3. This compound demonstrates potential in blocking tumor cell signaling pathways, thereby impeding tumor growth and progression. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting EGFR-related pathways. -
FLT3 Inhibitor
FLT3-IN-40 is a type I ATP-competitive inhibitor of FLT3, demonstrating an IC50 of 16.26 nM. This compound effectively reduces FLT3 autophosphorylation and downregulates ERK phosphorylation, thereby exhibiting significant antiproliferative activity, influencing cell cycle regulation, and promoting apoptosis. FLT3-IN-40 is particularly valuable for research applications focused on acute myeloid leukemia. -
VEGFR/Tyrosine Kinase Src Inhibitor
TG 100948 is a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and tyrosine kinase Src. This compound demonstrates significant biological activity by reducing retinal edema and retinal thickening, as well as eliminating bullous edema cysts in rat models of ischemic retinal vein occlusion. TG 100948 is valuable for research into the pathophysiology and potential treatments of ischemic retinal vein occlusion.
