Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Src Inhibitor
Hibarimicin G is a selective Src inhibitor derived from Microbispora rosea subsp. Hibaria. It exhibits potent activity against Src family tyrosine kinases, playing a crucial role in cell signaling pathways involved in cancer progression and metastasis. Hibarimicin G is utilized in research to elucidate the function of Src in various biological processes and to explore therapeutic strategies for targeting Src-mediated pathways in cancer treatment. -
Src Inhibitor
TOP1288 is a selective Src inhibitor, demonstrating potent activity against P38α, Src, and Syk kinases, with IC50 values of 116 nM, 24 nM, and 659 nM, respectively. This compound effectively inhibits the release of inflammatory cytokines from inflamed biopsies and myofibroblasts, making it a valuable tool for research on inflammation and related pathways. Its targeted action supports investigations into the modulation of kinase activity in various cellular contexts. -
c-Src Inhibtior
CGP062464 is a potent inhibitor of the tyrosine kinase c-Src, exhibiting an IC50 of less than 50 nM. This compound is primarily utilized in research related to osteoporosis and tumor-induced hypercalcemia, offering valuable insights into the signaling pathways involved in these conditions. Its selective inhibition of c-Src makes it a useful tool for investigating the role of this kinase in various biological processes. -
Src Inhibitor
Hibarimicin A is a selective Src tyrosine kinase inhibitor derived from Microbispora rosea subsp. hibaria. It effectively inhibits Src activity while sparing protein kinases A and C, making it a valuable tool for studying cellular signaling pathways involving Src. In addition to its role as a kinase inhibitor, Hibarimicin A exhibits moderate antibacterial activity against Gram-positive bacteria, with a minimum inhibitory concentration (MIC) ranging from 0.8 to 12.56 μg/mL, broadening its potential applications in microbiology and pharmacology research. -
Src SH2 Inhibitor
AP22408 is a potent nonpeptide inhibitor of the Src SH2 domain, exhibiting an IC50 value of 0.3 μM. This compound effectively inhibits osteoclast-mediated resorption of dentine in rabbits and demonstrates strong bone-targeting properties. In vivo studies reveal its antiresorptive activity in a parathyroid hormone-induced rat model, indicating potential applications in osteoporosis research and other bone-related diseases, including Paget’s disease, osteolytic bone metastasis, and malignancy-associated hypercalcemia. -
Src Inhibitor
Rhodomycin A is a potent Src inhibitor that modulates Src-related signaling pathways. This compound demonstrates significant biological activity by suppressing cancer cell proliferation, migration, invasion, and clonogenicity in vitro, as well as inhibiting tumor growth in vivo. Rhodomycin A is valuable for research applications targeting lung cancer and investigating the role of Src in tumor progression. -
Src Kinase Inhibitors
Saracatinib-d3 is a deuterium-labeled analog of Saracatinib and acts as an inhibitor of Src kinase. This compound exhibits significant anti-inflammatory properties, making it relevant in studies related to severe sepsis triggered by bacterial and microbial infections. Saracatinib-d3 is a valuable tool for research applications focused on Src kinase pathways and their implications in various disease states. -
Src Inhibitor
Hibarimicin C is a selective Src tyrosine kinase inhibitor that modulates cellular signaling pathways involved in various cancers. It exhibits significant specificity by inhibiting Src activity while leaving protein kinases A and C unaffected. In addition to its role in cancer research, Hibarimicin C displays moderate antibacterial activity against Gram-positive bacteria, with a minimum inhibitory concentration (MIC) ranging from 0.8 to 12.56 μg/mL. This compound is pertinent for studies in oncology and microbiology. -
Src Inhibitor
Hibarimicin B is a selective Src tyrosine kinase inhibitor that effectively disrupts Src activity while not interfering with protein kinase A or C. This compound demonstrates moderate antibacterial activity against Gram-positive bacteria, with a minimum inhibitory concentration (MIC) range of 0.8-12.56 μg/mL. Hibarimicin B is utilized in research applications focused on cancer cell signaling pathways and microbial resistance mechanisms. -
Src Inhibitor
Hibarimicin D is a selective inhibitor of the Src tyrosine kinase, effectively disrupting its enzymatic activity while sparing protein kinases A and C. In addition to its role as a Src inhibitor, Hibarimicin D exhibits moderate antibacterial properties against Gram-positive bacteria, with a minimum inhibitory concentration (MIC) ranging from 0.8 to 12.56 μg/mL. This compound offers valuable applications in research focused on cancer signaling pathways and antibacterial studies. -
TrkB Inhibitor
Cyclotraxin B is a selective inhibitor of the TrkB receptor, effectively crossing the blood-brain barrier. It inhibits brain-derived neurotrophic factor (BDNF) induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B exhibits notable analgesic and anxiolytic properties, making it a valuable tool for research into neurological disorders and pain management. -
TrkA Inhibitor
TrkA-IN-3 is a potent allosteric inhibitor of TrkA, exhibiting an IC50 of 22.4 nM. It demonstrates over 8000-fold selectivity for TrkA compared to TrkB and TrkC, making it a valuable tool for targeted studies. This compound is applicable in pain research, aiding in the exploration of neurogenic pain mechanisms and potential therapeutic interventions. -
Trk Receptor Inhibitor
GNF-8625 monopyridin-N-piperazine hydrochloride is a potent inhibitor of the Tropomyosin receptor kinase (Trk) family. This compound effectively disrupts the signaling pathways associated with Trk receptors, which are implicated in neurotrophic signaling and oncogenesis. GNF-8625 is utilized in research applications focused on neurobiology, cancer pharmacology, and targeted therapies to elucidate the role of Trk signaling in tumor growth and nerve regeneration. -
Trk Inhibitor
Utatrectinib (AZD-7451) is a selective and potent oral inhibitor of tropomyosin receptor kinases (Trk). By inhibiting TrkC activation, Utatrectinib effectively disrupts tumorigenic signaling pathways associated with various cancers. This compound is primarily utilized in research focused on neurotrophin receptor modulation and its implications in oncogenesis. -
Tyrosine Kinase Inhibitor
Paltimatrectinib is a potent tyrosine kinase inhibitor with an IC50 of less than 10 nM for tropomyosin receptor kinases A (TrkA). This compound demonstrates significant biological activity in inhibiting cell proliferation and migration associated with cancer and inflammatory diseases. Paltimatrectinib is applicable in research focused on therapeutic strategies for malignancies and inflammatory disorders. -
TrkA Inhibitor
TrkA-IN-4 is a potent allosteric inhibitor of TrkA, functioning as a proagent of TrkA-IN-3 with an IC50 value of 22.4 nM. This compound demonstrates significant antinociceptive effects, making it an important tool for research in pain modulation and neurobiology. Its orally active formulation enhances its utility in pharmacological studies exploring the role of TrkA in various pain-related pathways. -
TRK PROTAC Degrader
CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma. -
Nerve Growth Factor Receptor Antagonist
ALE-0540 is a nonpeptidic small molecule that acts as an antagonist of the nerve growth factor receptor. It effectively inhibits the binding of nerve growth factor (NGF) to the receptor tyrosine kinase A (TrkA) and the p75 neurotrophin receptor, with IC50 values of 5.88 μM and 3.72 μM, respectively. This compound is valuable for investigating the underlying mechanisms of pain and developing new therapeutic agents targeting pain pathways. -
Trk Receptor Inhibitor
TrkA-IN-1 is a selective inhibitor of the Tropomyosin-related kinase A (TrkA) receptor, demonstrating an IC50 of 99 nM in cell-based assays. This compound exhibits analgesic activity, making it valuable in research focused on pain pathways and neurobiology. TrkA-IN-1 can be utilized to explore the role of TrkA in various biological processes and disease models related to pain and neurodegeneration. -
TrkBR Activator
ENT-C225 is a potent activator of the TrkB neurotrophin receptor, known for its ability to enhance receptor signaling. This compound exhibits strong neuroprotective properties and favorable physicochemical characteristics, making it suitable for various research applications. Researchers may utilize ENT-C225 in studies focused on neurodegenerative diseases, synaptic plasticity, and neuronal growth. -
Negative Control
CG428-NEG is a negative control for TRK degradation assays. It serves to establish baseline responses in research studies examining the inhibition of cell growth and the modulation of TPM3-TRKA levels. This reagent is essential for validating experimental results involving TRK-targeted therapies and ensuring the specificity of TRK degradation effects. -
Stable Isotope
Amitriptyline-d3 hydrochloride is a deuterium-labeled derivative of amitriptyline, primarily targeting the serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET). It exhibits Ki values of 3.45 nM and 13.3 nM for human SERT and NET, respectively, and demonstrates weak binding to the dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Additionally, amitriptyline-d3 hydrochloride acts as an agonist for TrkA and TrkB receptors, exhibiting neurotrophic activity and contributing to its antidepressant effects. This stable isotope is valuable for metabolic studies and drug mechanism research. -
Trk Inhibitor
LPM4870108 is a potent pan-Trk inhibitor, targeting wild-type and mutant variants with IC50 values of 0.2 nM for TrkC, 2.4 nM for TrkA, 3.5 nM for TrkAG595R, and 2.3 nM for TrkAG667C. It demonstrates selectivity for Trk over ALK, with an IC50 of 182 nM. LPM4870108 exhibits significant anti-tumor activity, making it a valuable tool for studying Trk-related oncogenic signaling pathways and developing targeted cancer therapies. -
TRKA/C Inhibitor
TRK-IN-24 is a potent inhibitor of Trk receptors, specifically targeting TRKA, TRKC, TRKAG595R, TRKAG667C, and TRKAF589L, with IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM, respectively. This compound demonstrates significant antitumor activity in xenograft models, including BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C. Additionally, TRK-IN-24 effectively inhibits the proliferation of Ba/F3 cells harboring various single mutants, achieving IC50 values ranging from 1.43 to 47.56 nM. This makes TRK-IN-24 a valuable tool for research applications focused on targeted cancer therapies. -
TRK Inhibitor
Trk-IN-7 is a potent TRK inhibitor targeting TRKA, TRKB, and TRKC, with IC50 values ranging from 0.25 to 10 nM. Additionally, Trk-IN-7 demonstrates significant inhibitory activity against EML4-ALK and various ALK mutations, including G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A, with IC50 values ranging from 5 to 50 nM. This compound is valuable for research in neurotrophic signaling and cancer biology, particularly involving TRK and ALK pathways. -
TrkB Activator
TrkB activator-1 is a specific, orally bioavailable activator of tropomyosin receptor kinase B (TrkB) that effectively penetrates the blood-brain barrier. It demonstrates significant antidepressant properties by engaging the BDNF-TrkB-CREB signaling pathway, thereby enhancing neuroplasticity. This compound is valuable for research on neurological disorders, particularly in the study of depression and its underlying mechanisms. -
TrkB/C Modulator
PTX-BD10-2 is an orally active modulator of TrkB/C that demonstrates protective effects against basal forebrain cholinergic neuron (BFCN) degeneration. This compound has been shown to restore cholinergic neurite integrity and alleviate cholinergic neurite atrophy. PTX-BD10-2 serves as a valuable tool in research focused on Alzheimer's disease and related neurodegenerative disorders. -
TRK Inhibitor
Trk-IN-8 is a potent TRK inhibitor that exhibits IC50 values of 0.42 nM for TRKAa, 0.89 nM for TRKA(G595R), and 1.5 nM for TRKC(G623R). This compound is effective in selectively targeting Tropomyosin receptor kinase (TRK) signaling pathways, making it a valuable tool for research in cancer biology and therapeutic development. Its high selectivity and potency facilitate studies of TRK-related oncogenic processes and potential treatment strategies for TRK fusion-positive tumors. -
Trk Inhibitor
Trk-IN-20 is a potent inhibitor of Trk kinases, specifically targeting TrkA, TrkB, and TrkC with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively. By inhibiting the phosphorylation of these receptors, Trk-IN-20 effectively suppresses their kinase functions. This compound is valuable in research applications aimed at understanding neurotrophic signaling pathways and exploring therapeutic strategies for conditions related to Trk receptor dysregulation. -
TRK Inhibitor
GZ-389988 is a potent pan-TRK inhibitor that targets TRKA, TRKB, and TRKC with IC50 values of 0.3 nM, 0.1 nM, and 0.5 nM, respectively. It is valuable for the study of NTRK fusion-positive tumors, facilitating research into their biological mechanisms and potential therapeutic strategies. This compound supports the investigation of TRK-related pathways and their role in oncogenesis. -
RET/TRKA Inhibitor
RET/TRKA-IN-1 is a dual inhibitor targeting both RET and TRKA, with an IC50 value of 0.375 µM for RET. This reagent has demonstrated significant anti-proliferative effects on LC-2 and KM12 cell lines, exhibiting GI50 values of 0.72 µM and 0.25 µM, respectively. Additionally, RET/TRKA-IN-1 effectively induces cell cycle arrest at the G1 phase, making it a valuable tool for research on cancer biology and therapeutic development. -
TRK Inhibitor
TIY-7 is a selective and orally active inhibitor of tropomyosin receptor kinases (TRKs). It demonstrates potent enzyme inhibition with IC50 values of 2.9 nM for TRKA and as low as 0.2 nM for TRKCG696A, showcasing its efficacy against various TRK mutations. TIY-7 exhibits significant anti-tumor activity in mouse xenograft models, making it a valuable tool for research in cancer biology and targeted therapy development.
