Protein Tyrosine Kinases

Items 1451-1500 of 1870

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  1. VEGFR-2/c-Met Inhibitor

    VEGFR-2/c-Met-IN-1 is a potent dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and c-Met, with IC50 values of 138 nM and 74 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its dual mechanism of action allows for the exploration of therapeutic strategies aimed at inhibiting tumor growth and angiogenesis.
  2. VEGFR-2 Inhibitor

    VEGFR-2-IN-25 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 12.1 nM. This compound is primarily utilized in cancer research to investigate the role of angiogenesis in tumor progression and to evaluate therapeutic strategies targeting the VEGF signaling pathway. Its efficacy makes it a valuable tool for studying anti-tumor effects in various cancer models.
  3. PROTAC VEGFR2 Degrader

    PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis.
  4. VEGFR-2 Inhibitor

    VEGFR-2-IN-24 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), exhibiting an IC50 value of 0.22 µM. This compound is valuable in tumor research, facilitating the study of angiogenesis and the role of VEGFR-2 in various cancer models. Its efficacy makes it a useful tool for investigating therapeutic strategies targeting tumor vascularization.
  5. VEGFR-2 Inhibitor

    VEGFR-2-IN-65 is a selective inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2). It demonstrates high affinity and forms hydrogen bond interactions with Cys180 of the receptor. This compound has been shown to effectively inhibit tube formation in human umbilical vein endothelial cells (HUVECs), making it a valuable tool for investigating angiogenesis and vascular biology pathways. Research applications include the study of tumor angiogenesis and vascular disorders.
  6. FLuc/VEGFR Inhibitor

    GSK248233A is a dual inhibitor targeting FLuc and VEGFR2, exhibiting IC50 values of 1.03 μM and 2 nM, respectively. This compound also demonstrates activity against the AGC family of protein kinases. By inhibiting ATP-dependent and -independent luciferases, GSK248233A holds potential for applications in FLuc reporter assays and related biological research.
  7. VEGFR Inhibitor

    VEGFR-IN-7 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor (VEGFR), primarily involved in regulating angiogenesis. This compound demonstrates potential for modulating angiogenic processes and is particularly relevant in the study of cardiovascular diseases and related pathologies. Its ability to interfere with VEGFR signaling makes it a valuable tool for investigating therapeutic strategies aimed at vascular-related conditions.
  8. VEGFR Inhibitor

    VEGFR/PDGFR-IN-1 is a potent inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR) with an IC50 of 0.4 μM. This compound effectively inhibits angiogenesis in Human Umbilical Vein Endothelial Cells (HUVEC), demonstrating potential for application in tumor growth and metastasis research. Its targeted mechanism makes it a valuable tool for studying vascular-related pathologies and developing anti-cancer therapies.
  9. PDGFR Inhibitor

    cis-SU4312 is a potent inhibitor of the Platelet-Derived Growth Factor Receptor (PDGFR) and FLK-1, exhibiting IC50 values of 19.4 μM and 0.8 μM, respectively. Additionally, cis-SU4312 targets several other receptors, including EGFR, HER-2, and IGF-1R with IC50 values of 24.2 μM, 18.5 μM, and 10.0 μM, respectively. Due to its ability to cross the blood-brain barrier, cis-SU4312 is valuable in research applications related to cancer biology and neurobiology.
  10. SRC/Raf/VEGFR2 Inhibitor

    SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research.
  11. VEGFR Antagonist

    K-106 is a selective vascular endothelial growth factor receptor (VEGFR) antagonist that also inhibits neurotrophic tyrosine kinase receptors (NTRK). This compound exhibits significant biological activity in modulating angiogenesis and neuroprotection, making it a valuable tool for investigating retinal research and related therapeutic applications. Its dual inhibitory profile supports studies focused on vascular and neurological disorders.
  12. VEGFR Inhibitor

    VEGFR-IN-6 is an inhibitor of the vascular endothelial growth factor receptor (VEGFR), known for its ability to impede angiogenesis. This compound is particularly relevant in the study of tumor biology, where angiogenesis plays a critical role in tumor progression and metastasis. VEGFR-IN-6 serves as a valuable tool for researchers investigating the mechanisms of cancer and the development of anti-angiogenic therapies.
  13. VEGFR2 Kinase Inhibitor

    VEGFR2-IN-4 is a selective inhibitor of the VEGFR2 kinase, exhibiting a GI50 value of 0.7 nM. This compound demonstrates significant anti-angiogenic activity, making it a valuable tool for investigating the role of angiogenesis in various biological processes. VEGFR2-IN-4 is suitable for research applications related to rheumatoid arthritis and other angiogenesis-associated conditions.
  14. PDGFRβ Inhibitor

    SU16f is a potent and selective inhibitor of PDGFRβ, exhibiting IC50 values of 10 nM for PDGFRβ, 140 nM for VEGF-R2, and 2.29 μM for FGF-R1. By effectively neutralizing the PDGFRβ receptor, SU16f disrupts the supportive effects of gastric cancer-derived mesenchymal stem cells (GC-MSCs) conditioned medium on gastric cancer cell proliferation and migration. This compound is valuable for research applications focused on gastric cancer and the modulation of tumor microenvironments.
  15. PDGFR Inhibitor

    PDGFR Tyrosine Kinase Inhibitor III is a potent inhibitor of platelet-derived growth factor receptor (PDGFR), along with other kinases such as EGFR, FGFR, PKA, and PKC. This multikinase inhibitor plays a crucial role in modulating various signaling pathways involved in cellular proliferation and survival. Its application extends to the investigation of amyotrophic lateral sclerosis, providing insights into the underlying mechanisms of this neurodegenerative disorder. Researchers can employ this compound to explore therapeutic strategies targeting PDGFR and associated pathways.
  16. PDGFR Inhibitor

    WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR), effectively blocking PDGFR autophosphorylation with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. This compound significantly inhibits the proliferation and migration of pulmonary artery smooth muscle cells (PASMCs) by interfering with PDGF-BB-induced ERK1/2 phosphorylation, thus reducing collagen I synthesis and enhancing α-smooth muscle actin expression. WQ-C-401 is a valuable tool for studying mechanisms underlying pulmonary vascular remodeling and holds potential for research in pulmonary arterial hypertension.
  17. PDGFR Antagonist

    CT52923 is a selective antagonist of the platelet-derived growth factor receptor (PDGFR) and acts as an ATP-competitive inhibitor. This compound demonstrates significant biological activity relevant to a range of pathological conditions, including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and certain cancers. CT52923 can be utilized to explore therapeutic pathways and mechanisms involved in these diseases.
  18. PDGFr Inhibitor

    PDGFR-IN-2 is a 4-phenoxyquinoline derivative that acts as a selective inhibitor of the platelet-derived growth factor receptor (PDGFr) with an IC50 value of 0.20 μM. By targeting PDGFr tyrosine kinase activity, PDGFR-IN-2 effectively disrupts downstream signaling pathways associated with cell proliferation and migration. This compound is valuable for research applications investigating the role of PDGFr in various pathological conditions, including cancer and fibrotic diseases.
  19. PDGFR Inhibitor

    DMPQ dihydrochloride is a selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ), exhibiting an IC50 of 80 nM. This compound demonstrates significant potential in research applications focused on PDGFRβ-mediated signaling pathways, which are implicated in a variety of pathological conditions, including cancer and fibrosis. Its potency and selectivity make DMPQ dihydrochloride a valuable tool for investigating the role of PDGFRβ in cellular processes and therapeutic interventions.
  20. PDGFR Inhibitor

    AG 370 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), exhibiting potent activity against PDGF-induced mitogenesis with an IC50 of 20 μM. Additionally, AG 370 demonstrates weak inhibitory effects on the epidermal growth factor receptor (EGFR). This compound is valuable for research applications focused on signaling pathways related to cell proliferation and cancer biology.
  21. PDGFR-α Inhibitor

    PDGFRα kinase-IN-2 is a potent inhibitor of the platelet-derived growth factor receptor alpha (PDGFR-α) with an IC50 of 2.1 nM. This compound exhibits significant anticancer activity against HT-29 human colon cancer cells, with an IC50 of 1.48 μM. Additionally, PDGFRα kinase-IN-2 demonstrates anti-angiogenic properties in zebrafish models while exhibiting low embryonic lethality. It is a valuable tool for research focused on colon cancer and the mechanisms of anti-angiogenesis.
  22. TGFβRI/PDGFRα Inhibitor

    BI-4659 is a dual inhibitor of TGFβRI and PDGFRα, exhibiting IC50 values of 19 nM and 99 nM, respectively. This compound effectively inhibits the kinase activities of both receptors, thereby blocking downstream TGFβRI signaling and reducing Smad2/3 phosphorylation without impacting TGF-β1 expression. BI-4659 is suitable for research applications in pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury studies.
  23. PDGFR Fragment

    PDGFR Y1021 peptide (non-phosphorylation) is a specific non-phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR). This peptide effectively inhibits the association of PLCγ with PDGFR via the PLCγ SH2 domain, thereby blocking the mitogenic response. It serves as a valuable tool in research focused on signaling pathways involving PDGFR and its role in cell growth and proliferation.
  24. PDGFRA Inhibitor

    GSK190937 is a type II inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA), exhibiting notable antimalarial activity. This compound effectively inhibits hemozoin formation in malaria parasites, leading to the accumulation of free hemoglobin. GSK190937 demonstrates IC50 values of 0.22 μM, 0.59 μM, and 0.25 μM against Plasmodium falciparum strains NF54, K1, and Dd2, respectively. Additionally, it has an IC50 of 25 μM for CHO cells, making it a valuable tool for malaria research.
  25. PDGFR Fragment

    PDGFR Y1021 peptide (phosphorylation) is a phosphorylated fragment of the platelet-derived growth factor receptor (PDGFR) that facilitates the binding of phospholipase C-gamma (PLCγ) through its SH2 domains. This interaction enhances the production of inositol phosphates and stimulates mitogenic responses. The peptide serves as a valuable tool for research investigating PDGFR signaling pathways and their roles in cellular proliferation and differentiation.
  26. PDGFR Inhibitor

    KN1022 is a selective inhibitor of the phosphorylation of platelet-derived growth factor receptor (PDGFR), with an IC50 value of 0.24 μM. This compound effectively modulates PDGFR signaling pathways, making it a valuable tool for investigating the role of PDGFR in various cellular processes. It is particularly relevant for research in cancer biology, fibrosis, and other diseases associated with abnormal PDGFR activity.
  27. PDGFR Inhibitor

    Sch 13835 is a selective inhibitor of the platelet-derived growth factor receptor (PDGFR), which plays a critical role in cellular processes such as proliferation, differentiation, and survival. This compound exhibits significant inhibitory activity against PDGFR, making it a valuable tool for studying pathways involved in cancer and fibrosis. Its applications include investigating the role of PDGFR in tumor growth and exploring therapeutic strategies for conditions driven by aberrant PDGFR signaling.
  28. PDGFR-βInhibitor

    Tyrphostin AG1433 hydrochloride is a specific and potent inhibitor of PDGFR-β, with additional activity against KDR/Flk-1. It functions as an angiogenesis inhibitor, making it valuable for research into vascular biology and related pathologies. This compound is suitable for studies focused on cancer, fibrosis, and other diseases where angiogenesis plays a critical role.
  29. Src Inhibitor

    Saracatinib difumarate is a selective Src inhibitor, effectively targeting multiple Src family kinases, including c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk, with IC50 values ranging from 2.7 to 11 nM. This compound demonstrates significant potential in modulating signaling pathways associated with cancer and other diseases driven by Src family kinases. It is commonly utilized in research focusing on cancer biology, cell signaling, and the development of targeted therapies.
  30. Src

    3'-Demethylnobiletin is a flavonoid derivative that targets the Src kinase. This compound has demonstrated notable anticancer activity by inhibiting tumor angiogenesis through modulation of Src, FAK, and STAT3 signaling pathways. It is useful in cancer research for studying mechanisms of tumor growth and progression.
  31. RET/BRAF/S6K/Src Inhibitor

    AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases.
  32. Src SH2 Inhibitor

    pYEEI is a phosphotyrosine-containing tetrapeptide that selectively inhibits the Src SH2 domain with a Kd of 100 nM and an IC50 of 6.5 μM. This compound is pivotal for studying the role of Src signaling pathways in cancer biology and can aid in the development of targeted therapies. Its ability to modulate Src activity makes pYEEI a valuable tool for researchers investigating tumorigenesis and related processes.
  33. SRC-3 Inhibitor

    SRC-3-IN-2 is a selective inhibitor of steroid receptor coactivator 3 (SRC-3), demonstrating potent antitumor activity. This compound is utilized in research focusing on cancer biology and hormone receptor signaling pathways. Its ability to modulate SRC-3 activity makes it a valuable tool for studying SRC-3's role in tumorigenesis and therapeutic resistance.
  34. Src inhibitor

    Fenlean is a natural squamosamide derivative that acts as a Src tyrosine kinase inhibitor. It demonstrates the ability to inhibit over-activated microglia, thereby providing protective effects on dopaminergic neurons. Its anti-inflammatory properties support its potential application in the study and treatment of neuroinflammation in models of Parkinson's disease.
  35. Control Substrate For c-Src Assay

    Tyrosine Kinase Peptide 1 serves as a control substrate specifically designed for c-Src assay applications. Its primary mechanism involves interacting with c-Src kinase, facilitating the assessment of kinase activity. This peptide is critical for validating experimental conditions and ensuring accurate measurement of c-Src-mediated phosphorylation events in biological research.
  36. Src Inhibitor

    LDDN-0003499 is a Src family tyrosine kinase inhibitor that exhibits anti-inflammatory properties. This compound effectively reduces both basal and amyloid-beta (Aβ)-stimulated levels of active phosphorylated Lyn and Src kinases, leading to diminished secretion of pro-inflammatory cytokines such as TNFα and IL-6 in microglial cells. LDDN-0003499 is particularly valuable for research focused on the pathophysiology of Alzheimer's disease.
  37. pp60c-src SH2 Domain Inhibitor

    N-Acetyl-O-phosphono-Tyr-Glu dipentylamide is an inhibitor of the pp60c-src SH2 domain. Its primary biological activity involves modulating signaling pathways associated with cancer progression and metastasis. This compound is valuable for research applications aimed at understanding Src family tyrosine kinases and developing targeted cancer therapies.
  38. p60v-src Inhibitor

    P60v-src(137-157) is a synthetic peptide specifically designed to inhibit the tyrosine kinase activity of the p60v-src protein, exhibiting an IC50 value of 7.5 μM. This peptide serves as a valuable tool in research related to cancer biology and signal transduction pathways, allowing for investigation into the role of p60v-src in cellular processes. Its inhibition capability makes it ideal for studies assessing the effects of p60v-src on cell growth, differentiation, and oncogenesis.
  39. Src Inhibitor

    Antiallergic agent-1 is a Src-family kinase inhibitor, demonstrating potential as a lead compound for the development of novel antiallergic therapies. This compound features an alkyne functional group that allows it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications. Its unique properties support research into allergic response mechanisms and therapeutic interventions.
  40. Src Inhibitor

    LCB 03-0110 is a thienopyridine derivative that serves as a potent inhibitor of Src family tyrosine kinases and pan-discoidin domain receptors. This compound is effective in suppressing scar formation by inhibiting the activation of fibroblasts and macrophages. Its key biological activity makes it a valuable tool for research applications focused on tissue repair and fibrosis.
  41. Src Inhibitor

    KL-1156 is a selective Src inhibitor that demonstrates potent activity with an IC50 of 1 nM and a Ki of 540 pM. This compound effectively inhibits T cell proliferation, with an IC50 value of 262 nM. KL-1156 is useful for research applications focused on immune response modulation and the investigation of Src-related signaling pathways in cancer and other diseases.
  42. Src

    TOP1210 is a selective tyrosine kinase inhibitor that targets Src, P38α, and Syk kinases. It demonstrates significant anti-inflammatory activity by effectively reducing the release of proinflammatory cytokines from various immune and inflammatory cell types, including peripheral blood monocytes and primary macrophages. TOP1210 shows promise in research applications related to inflammatory conditions, particularly ulcerative colitis, by offering a broader therapeutic potential through its multi-kinase inhibition profile, which may enhance the modulation of autoimmune responses.
  43. Src Inhibitor

    DC-Srci-6649 is a selective inhibitor of c-Src kinase, designed to impede its phosphorylation and maintain c-Src in an inactive conformation. This compound demonstrates significant potential in studies of cancer biology and cell signaling, making it a valuable tool for investigating the role of c-Src in tumorigenesis and other pathological conditions. Researchers can utilize DC-Srci-6649 to explore therapeutic strategies targeting Src-mediated pathways.
  44. Src Inhibitor

    LCB 03-0110 dihydrochloride is a potent inhibitor of Src family tyrosine kinases, functioning primarily by targeting their catalytic activity. This compound exhibits significant biological activity, making it valuable for research in cancer biology and cellular signaling pathways. It is particularly useful for studying the role of Src in tumorigenesis and metastasis, as well as in assessing therapeutic strategies for Src-related disorders.
  45. src SH3-SH2:Phosphoprotein Inhibitor

    Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is a high-affinity pentapeptide targeting the src SH2 domain, exhibiting an IC50 of approximately 1 µM. This compound serves as an effective inhibitor of src SH3-SH2:phosphoprotein interactions. It is valuable in research applications focused on signaling pathways and protein-protein interactions involving src family kinases.
  46. RET/BRAF/S6K/Src Inhibitor

    AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models.
  47. Src SH2 Domain Inhibitor

    AP-22161 is a selective inhibitor of the Src SH2 domain, exhibiting an IC50 of 0.24 µM. It demonstrates over 120-fold selectivity against Yes SH2 (IC50 = 29.38 µM) and ZAP SH2 (IC50 = 421.86 µM). This compound effectively inhibits Src-dependent cellular functions and reduces osteoclast resorptive activity, making it a valuable tool for research in osteoporosis and related bone disorders.
  48. Src Family Kinases Inhibitor

    PP2 Analog is an ATP-competitive inhibitor targeting Src family kinases, demonstrating IC50 values of 0.22 µM for Lck, 0.15 µM for Src, 2.68 µM for Kdr, and 7 µM for Tie-2. This compound is utilized in research for its ability to modulate kinase activity, aiding in the study of signal transduction pathways and cancer biology. It is particularly useful in delineating the roles of Src family kinases in various cellular processes and disease states.
  49. pp60c-src Substrate

    p60c-src substrate II is a specific pentapeptide substrate designed for the tyrosine kinase pp60c-src. This substrate facilitates the study of tyrosine phosphorylation mediated by pp60c-src, enabling key insights into its role in cell signaling pathways. It is ideally suited for research applications involving cancer biology and other cellular processes regulated by pp60c-src activity.
  50. Src SH2 Ligand

    ISO24 is a potent ligand targeting the Src SH2 domain, exhibiting an IC50 of 4.4 mM as determined by BIAcore assays. This compound provides valuable insights into Src signaling pathways, making it suitable for research applications in cancer biology and signal transduction studies. Its specificity for the Src SH2 domain enhances its utility in exploring protein-protein interactions and downstream signaling cascades.

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