Protein Tyrosine Kinases

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  1. CSF1R Inhibitor

    CSF1R-IN-4 is a selective inhibitor of the colony-stimulating factor 1 receptor (CSF1R). This compound plays a critical role in modulating macrophage survival and differentiation by targeting the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 has been shown to influence the interaction between tumor-associated macrophages (TAMs) and glioma cells, making it a valuable tool for cancer research. Its potential applications include studying the tumor microenvironment and the immune response in various malignancies.
  2. CSF1R Inhibitor

    CSF1R-IN-25 is a selective inhibitor of the Colony Stimulating Factor 1 Receptor (CSF1R). This compound demonstrates significant potential in modulating biological processes related to cancer, inflammation, and neurodegeneration. It serves as a valuable tool for researchers investigating the therapeutic implications of CSF1R inhibition in these areas.
  3. CSF1R Inhibitor

    CSF1R-IN-19 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R). It modulates the interaction between tumor-associated macrophages and glioma cells, influencing the exchange of inflammatory factors. This compound is significant for cancer research, particularly in understanding the tumor microenvironment and exploring therapeutic strategies targeting CSF1R.
  4. Axl/Mer/CSF1R Inhibitor

    Axl/Mer/CSF1R-IN-1 is an inhibitor of Axl/Mer receptor tyrosine kinases and CSF1R, demonstrating a binding affinity with Kds of less than 0.1 μM. This compound is valuable for research focused on the modulation of signaling pathways related to cancer, inflammation, and immune response. Its ability to precisely inhibit these targets makes it a useful tool in studies investigating the roles of Axl, Mer, and CSF1R in various biological processes.
  5. CSF-1R Inhibitor

    CSF1R-IN-8 is a potent inhibitor of colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.012 μM. This compound exhibits significant biological activity in modulating CSF-1R signaling pathways, which are crucial for monocyte and macrophage differentiation and function. CSF1R-IN-8 is applicable in research focusing on immunology, cancer therapy, and the study of tumor microenvironments.
  6. CSF1R Inhibitor

    CSF1R-IN-13 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF1R). As a crucial growth factor, CSF-1 modulates the development of bone marrow progenitor cells, monocytes, and macrophages, influencing immune response and cancer progression. This compound serves as a valuable research tool for investigating CSF1R's role in cancer therapies and related disease mechanisms.
  7. CSF-1R Inhibitor

    CSF1R-IN-10 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF-1R) with an IC50 of 0.005 μM. This compound effectively disrupts CSF-1R signaling, which is crucial for the regulation of macrophage proliferation and differentiation. CSF1R-IN-10 is valuable for research applications focusing on inflammatory diseases, cancer, and the immune response, where modulation of macrophage activity is of interest.
  8. CSF-1R Inhibitor

    Edicotinib hydrochloride is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF-1R), demonstrating an IC50 of 3.2 nM. This compound is brain penetrant and orally bioavailable, showing minimal off-target effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib hydrochloride effectively limits microglial expansion, attenuating neurodegeneration in preclinical models. Its unique profile offers potential applications in research related to Alzheimer's disease and rheumatoid arthritis.
  9. CSF1R Inhibitor

    CSF1R-IN-21 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R) with an IC50 value of 31 nM. This compound effectively inhibits CSF1R auto-phosphorylation, making it a valuable tool for investigating the role of CSF1R in neurodegenerative diseases. CSF1R-IN-21 can be utilized in research studies aimed at understanding the molecular mechanisms underlying these conditions and exploring potential therapeutic interventions.
  10. CSF1R Inhibitor

    CSF1R-IN-6 is a potent inhibitor of the colony-stimulating factor 1 receptor (CSF1R), which plays a critical role in regulating macrophage survival and differentiation through the CSF-1/CSF1R signaling pathway. This compound modulates the exchange of inflammatory mediators between tumor-associated macrophages (TAMs) and glioma cells, contributing to the understanding of tumor microenvironment interactions. CSF1R-IN-6 is a valuable tool for cancer research, particularly in elucidating the mechanisms underlying tumor progression and immune evasion.
  11. CSF-1R Inhibitor

    CSF1R-IN-20 is a potent inhibitor of the colony stimulating factor 1 receptor (CSF-1R), exhibiting an IC50 value of 467 nM. This compound effectively inhibits CSF-1R auto-phosphorylation, thereby interfering with downstream signaling pathways. It is primarily utilized in research applications focused on understanding macrophage biology and associated diseases, including cancer and inflammatory disorders.
  12. CSF1R Inhibitor

    CSF1R-IN-15 is a selective inhibitor of the colony-stimulating factor-1 receptor (CSF1R), a membrane-bound tyrosine kinase primarily expressed in macrophages. This compound disrupts CSF1R signaling, which is essential for macrophage differentiation, proliferation, and survival, by targeting its interaction with colony-stimulating factor-1 (CSF-1) and interleukin-34. CSF1R-IN-15 is valuable for research applications focused on macrophage biology and associated pathologies, including cancer, inflammation, and autoimmune diseases.
  13. IGFBP Inhibitor

    NBI-31772 is a non-selective inhibitor of insulin-like growth factor binding proteins (IGFBPs) with a Ki value of 47 nM. This compound exhibits neuroprotective properties and significantly reduces infarct volume during cerebral ischemia. Additionally, NBI-31772 enhances proteoglycan synthesis in osteoarticular chondrocytes and has been shown to amplify the effects of IGF3 on oocyte maturation in zebrafish. Its diverse biological activities make it a valuable tool for research in neuroprotection and chondrocyte biology.
  14. IGF-I Receptor Inhibitor

    JB-1 is a selective inhibitor of the IGF-I receptor, specifically designed to compete with IGF-I for binding at the IGF-1R site, without affecting IGF-II. This compound effectively blocks receptor autophosphorylation, leading to an increase in soluble VEGFR-1 levels. JB-1 demonstrates significant efficacy in normalizing retinal abnormalities, particularly in the context of reducing retinal neovascularization. Its application is particularly relevant for research focused on oxygen-induced retinopathy.
  15. IGF-1 Receptor Kinase Inhibitor

    AG 538 is a potent competitive inhibitor of the IGF-1 receptor kinase, with an IC50 value of 400 nM. This compound effectively blocks IGF-1 signaling pathways, which play a critical role in cell proliferation and survival. Due to its inhibitory action, AG 538 is valuable in research applications investigating cancer growth, metabolic diseases, and other conditions linked to dysregulated IGF-1 signaling.
  16. IGF-1R Inhibitor

    IGF-1R inhibitor-2 is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R). This compound downregulates IGF-1R activity, which can reverse the transformed phenotype of tumor cells, thereby increasing their susceptibility to apoptosis. It is valuable for research applications focused on cancer biology and therapeutic strategies targeting IGF signaling pathways.
  17. IGF-1R/PI5P4Kα Inhibitor

    I-OMe-Tyrphostin AG 538 is a selective inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. This compound effectively disrupts IGF-1R-mediated signaling pathways and demonstrates preferential cytotoxicity towards nutrient-deprived PANC1 cells. Additionally, I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), exhibiting an IC50 value of 1 μM. It is valuable for research applications focused on cancer biology and metabolic stress responses.
  18. IGF-1R/SRC Inhibitor

    IGF-1R/SRC-IN-1 is a selective inhibitor targeting insulin-like growth factor 1 receptor (IGF-1R) and SRC. This compound demonstrates an IC50 value of 63 μM for IGF-1R, making it a valuable tool in the study of signal transduction pathways involved in cancer and metabolic disorders. Its application extends to evaluating the role of IGF-1R and SRC in cellular proliferation, differentiation, and survival, providing insights into potential therapeutic interventions for related diseases.
  19. IGF-IR Inhibitor

    AZ12253801 is an ATP-competitive inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), demonstrating approximately 10-fold selectivity over the insulin receptor. It exhibits potent inhibition of IGF-1R-mediated proliferation in 3T3 mouse fibroblasts transfected with human IGF-1R, with an IC50 value of 17 nmol/L. Additionally, AZ12253801 shows reduced activity against epidermal growth factor receptor (EGFR)-driven proliferation, with an IC50 of 440 nmol/L. Its characteristics make it a valuable tool for investigating anti-tumor mechanisms and IGF-1R signaling pathways in cancer research.
  20. IGF1R Inhibitor

    IGF-1R inhibitor-3 is an allosteric inhibitor targeting insulin-like growth factor receptor 1 (IGF-1R) kinase, demonstrating an IC50 of 0.2 μM. This compound is instrumental in investigating IGF-1R signaling pathways and its role in various cancers and metabolic disorders. It has potential applications in cancer research, where modulation of the IGF-1R pathway may influence tumor growth and progression.
  21. IGF-1R Inhibitor

    BMS-577098 is an orally bioavailable inhibitor of the insulin-like growth factor-1 receptor (IGF-1R), displaying an IC50 of 0.016 μM. This ATP-competitive compound demonstrates significant anti-tumor activity, making it a valuable tool in cancer research. Its inhibition of IGF-1R can aid in the exploration of therapeutic strategies targeting tumor growth and progression.
  22. IGF-1R Inhibitor

    IGF-1R Inhibitor-5 is a selective inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 of 6 μM. This compound exhibits significant potential in cancer research by modulating IGF-1R signaling pathways, which are implicated in various malignancies. Its application may provide insights into tumor growth and progression mechanisms, making it a valuable tool for studies in oncology.
  23. IGF-1R Inhibitor

    IGF-1R inhibitor-4 is a potent inhibitor of insulin-like growth factor 1 receptor (IGF-1R), demonstrating an inhibition rate of 63% at a concentration of 10 μM. This compound is valuable in cancer research, as it interferes with IGF-1 signaling pathways that contribute to tumor cell proliferation and survival. Researchers can utilize IGF-1R inhibitor-4 to explore therapeutic strategies targeting IGF-1R in various malignancies.
  24. IGF-1R Inhibitor

    BMS 695735 is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting an IC50 of 0.034 μM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. It is suitable for studies investigating IGF-1R's role in tumorigenesis and for assessing potential therapeutic interventions targeting this receptor.
  25. VEGFR Inhibitor

    Aflibercept (VEGF Trap) acts as a soluble decoy receptor targeting vascular endothelial growth factor (VEGF) and inhibiting VEGF receptor (VEGFR) signaling. By fusing the immunoglobulin domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1, Aflibercept effectively diminishes VEGF-mediated biological processes. This reagent is primarily utilized in research related to age-related macular degeneration (AMD) and cardiovascular disease, facilitating studies on angiogenesis and vascular permeability.
  26. VEGFR inhibitor

    Tivozanib hydrochloride hydrate is a selective inhibitor targeting vascular endothelial growth factor receptors (VEGFR)-1, 2, and 3, with IC50 values of 30 nM, 6.5 nM, and 15 nM, respectively. This orally active compound demonstrates significant antitumor efficacy, making it a valuable tool for cancer research. Tivozanib hydrochloride hydrate is primarily utilized in studies focusing on angiogenesis and tumor proliferation, contributing to the advancement of targeted cancer therapies.
  27. VEGFR Inhibitor

    AAL993 is a potent inhibitor of Vascular Endothelial Growth Factor Receptors (VEGFR) with IC50 values of 130 nM for VEGFR1, 23 nM for VEGFR2, and 18 nM for VEGFR3. This compound selectively targets VEGFRs while showing reduced inhibition of other tyrosine kinases. AAL993 exhibits significant antiangiogenic and antitumor activities, making it a valuable tool for cancer research and studies focused on tumor vasculature modulation.
  28. VEGFR3 inhibitor

    VEGFR-3-IN-1 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) with an IC50 of 110.4 nM. It effectively inhibits the proliferation and migration of human dermal lymphatic endothelial cells (HDLEC), as well as breast cancer cell lines MDA-MB-231 and MDA-MB-436, by disrupting the VEGFR3 signaling pathway. This compound demonstrates significant potential in breast cancer research and therapies targeting lymphatic endothelial function.
  29. Eph-Ephrin Inhibitor

    UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that targets Eph-ephrin interactions. By inhibiting the interaction between VEGFR2 and its ligand, vascular endothelial growth factor, UniPR1331 effectively dampens autophosphorylation, subsequent signaling, and pro-angiogenic activation in endothelial cells. This compound demonstrates significant anti-angiogenic, anti-cancer, and anti-inflammatory properties, making it suitable for research applications in cancer and inflammation, including glioma and colitis.
  30. VEGFR Inhibitor

    DMH4 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), demonstrating potent activity with an IC50 of 0.16 µM. This reagent is valuable for research applications targeting angiogenesis and tumor growth, allowing for the investigation of cancer biology and potential therapeutic interventions.
  31. VEGFR2/Tie-2 Inhibitor

    TIE-2/VEGFR-2 kinase-IN-2 is a potent dual inhibitor of the Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and the Tyrosine kinase with immunoglobulin-like and EGF-like domains 2 (Tie-2), exhibiting pIC50 values of 8.61 and 8.56, respectively. This compound serves as an effective anti-angiogenic agent, making it a valuable tool for cancer research. Its ability to inhibit both targets can provide insights into tumor vascularization and growth.
  32. VEGFR2 Inhibitor

    VEGFR-2-IN-5 hydrochloride is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), a critical target involved in angiogenesis and tumor growth. This compound exhibits strong biological activity in inhibiting VEGFR-2 signaling, making it useful for research focused on cancer biology and vascular biology. Its application extends to the study of tumor microenvironments and potential therapeutic strategies targeting angiogenesis in various malignancies.
  33. VEGFR Inhibitor

    Ziv-aflibercept is a soluble vascular endothelial growth factor receptor (VEGFR) inhibitor. It demonstrates significant anti-angiogenic activity by blocking the interaction between VEGF and its receptors, thereby inhibiting endothelial cell proliferation and migration. This compound is primarily investigated for its therapeutic potential in metastatic colorectal carcinoma and various retinal diseases, offering insights into the modulation of tumor growth and ocular pathologies.
  34. VEGFR2 Inhibitor

    Rhamnazin is an orally active inhibitor of VEGFR2 signaling, exhibiting an IC50 of 4.68 μM against VEGFR2 kinase. This compound demonstrates significant antiangiogenic activity and antitumor efficacy, making it a valuable tool in cancer research. Additionally, Rhamnazin possesses antioxidant and anti-inflammatory properties, further broadening its potential applications in biological studies.
  35. VEGFR Inhibitor

    5α-Hydroxycostic acid is a natural eudesmane-type sesquiterpene that functions as a VEGFR inhibitor. It exhibits notable anti-angiogenic properties, effectively inhibiting the migration of breast cancer cells by modulating the VEGF/VEGFR2 and Ang2/Tie2 signaling pathways. This compound is valuable for research applications focused on cancer biology and therapeutic development targeting vascular endothelial growth factor receptors.
  36. VEGFR2/Tie-2 Inhibitor

    GW768505A free base is a potent dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) and Tie-2, exhibiting a pIC50 of 7.81 for VEGFR2. This compound demonstrates significant anti-angiogenic activity, making it valuable for research applications in cancer biology and therapeutic angiogenesis. It can be utilized in studies aimed at elucidating the roles of VEGFR2 and Tie-2 in various pathological conditions.
  37. VEGFR Inhibitor

    Bevasiranib sodium is a small interfering RNA (siRNA) targeting the vascular endothelial growth factor receptor (VEGFR). By silencing the genes responsible for VEGF production, it plays a crucial role in the inhibition of choroidal neovascularization (CNV), a significant factor in the development of wet age-related macular degeneration (wet AMD). This reagent is essential for research into therapeutic approaches for retinal diseases and the modulation of angiogenic processes.
  38. VEGFR-2 Inhibitor

    VEGFR-2-IN-37 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). Exhibiting an inhibition rate of approximately 56.9% at 200 μM, this compound demonstrates the potential to hinder the proliferation of human umbilical vein endothelial cells (HUVECs). It is an essential tool for researchers investigating angiogenesis and related vascular processes.
  39. VEGFR-2 Inhibitor

    VEGFR-2-IN-29 is an inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), demonstrating an IC50 of 16.5 nM. This compound effectively modulates angiogenesis and vascular permeability by inhibiting VEGFR-2 signaling. VEGFR-2-IN-29 is valuable in research related to tumor vasculature, cancer biology, and potential therapeutic interventions for diseases characterized by aberrant angiogenesis.
  40. VEGFR2 Inhibitor

    VEGFR-2-IN-6 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR2), an essential target in the modulation of angiogenesis. This compound demonstrates significant biological activity in inhibiting endothelial cell proliferation and tube formation. It is primarily utilized in research concerning cancer therapeutics and other conditions where neovascularization plays a critical role.
  41. TIE-2/VEGFR-2 Inhibitor

    TIE-2/VEGFR-2 kinase-IN-1 is a potent inhibitor targeting the TIE-2 and VEGFR-2 kinases, which are critical regulators of angiogenesis. This compound is instrumental in researching diseases characterized by abnormal blood vessel formation, including various cancers and diabetic retinopathy. Its application facilitates the exploration of therapeutic strategies aimed at modulating angiogenic processes and offers insights into the underlying mechanisms of angiogenesis-related pathologies.
  42. VEGFR/PDGFR Inhibitor

    BMS-605541 is a selective, orally active inhibitor targeting VEGFR-2 kinase, exhibiting an IC50 of 23 nM and a Ki of 49 nM. It also inhibits Flk-1, VEGFR-1, and PDGFR-β with IC50 values of 40 nM, 400 nM, and 200 nM, respectively. This reagent is valuable for cancer research, aiding in the study of angiogenesis and tumor progression.
  43. VEGFR2 Inhibitor

    (Z)-FeCP-oxindole is a selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR2), exhibiting an IC50 value of 200 nM. Additionally, it can significantly inhibit VEGFR1 and PDGFRα or β at concentrations of 10 μM. This compound demonstrates notable anticancer activity against B16 murine melanoma cell lines, with an IC50 of less than 1 μM, making it a valuable tool for cancer research and therapeutic studies.
  44. VEGFR2 Inhibitor

    VEGFR2-IN-7 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), a key regulator in angiogenesis. This compound demonstrates potent anticancer activity by interrupting the signaling pathways involved in tumor-associated blood vessel formation. VEGFR2-IN-7 is valuable for research applications targeting tumor vasculature and studying the role of angiogenesis in cancer progression.
  45. Lck/Src/KDR/VEGF2R/Tie-2/BLK/Csk/Fyn/Lyn Inhibitor

    RK-20448 is an ATP-competitive inhibitor targeting Lck, Src, KDR/VEGF2R, and Tie-2, demonstrating IC50 values of 0.24, 1.19, 10.74, and 5.85 µM, respectively. Additionally, it inhibits BLK, Csk, Fyn, and Lyn, with IC50 values of 0.37, 4.27, 2.03, and 0.43 µM, respectively. This compound is valuable for research involving signal transduction pathways mediated by receptor tyrosine kinases and may contribute to studies on cancer and vascular biology.
  46. VEGFR Inhibitor

    Tivozanib hydrate is a selective inhibitor of vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), displaying IC50 values of 30 nM, 6.5 nM, and 15 nM, respectively. This orally active compound demonstrates significant antitumor efficacy, making it a valuable tool for research focused on tumor angiogenesis and vascular biology. Its selectivity and potency facilitate investigations into VEGFR-related pathways and their implications in cancer treatment.
  47. VEGFR-2 Inhibitor

    VEGFR-2-IN-21 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting an IC50 of 0.10 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in oncology and vascular biology. Its ability to modulate VEGFR-2 signaling can aid in the investigation of tumor growth and metastasis, as well as facilitate the development of targeted therapies.
  48. VEGFR2 Inhibitor

    VEGFR-2-IN-35 is a potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting an IC50 value of 37 nM. This compound demonstrates significant anti-proliferative effects on MCF-7 and HCT 116 cancer cell lines, with IC50 values of 10.56 µM and 7.07 µM, respectively. VEGFR-2-IN-35 is suitable for research applications focused on angiogenesis and cancer cell proliferation.
  49. hCA/VEGFR-2 Inhibitor

    hCA/VEGFR-2-IN-3 is a potent inhibitor targeting cancer-associated human carbonic anhydrases (hCAs) IX and XII, as well as vascular endothelial growth factor receptor 2 (VEGFR-2). It demonstrates a VEGFR-2 inhibition with an IC50 of 358 nM and shows strong binding affinity to hCA IX with a Ki of 4.2 nM, as well as significant binding to hCA II, hCA I, and hCA XII. This compound exhibits antiproliferative properties in VEGFR-2-overexpressing breast cancer cells, making it valuable in cancer research and potential therapeutic applications.
  50. EGFR Inhibitor

    EGFR-IN-26 is a selective inhibitor of the epidermal growth factor receptor (EGFR), derived from patent WO2019162323A1, compound I-028. This compound significantly impedes EGFR activity, making it a valuable tool for investigating its role in cancer biology. It is applicable in cancer research, particularly in studies focused on targeting EGFR signaling pathways to develop novel therapeutic strategies.

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