Catalog No.
Product Name
Application
Product Information
Citations
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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. -
hTrkA Inhibitor
hTrkA-IN-2 is a selective allosteric inhibitor of human TrkA with an IC50 of 3.9 nM. This compound demonstrates the ability to modulate TrkA activity, making it valuable for studies investigating neurotrophic signaling pathways. hTrkA-IN-2 is suitable for research applications focused on neurobiology, potential therapeutic strategies for neurodegenerative diseases, and the exploration of pain mechanisms. -
TRKA Antagonist
Pegcantratinib is a selective TRKA antagonist that also exhibits activity against TRKB and TRKC. This compound is valuable for research into CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, including psoriasis and associated pruritus. Its targeted inhibition of TRK receptors makes it a promising tool for studying the underlying mechanisms of these conditions. -
TRK Inhibitor
TRK-IN-28 is a potent TRK inhibitor that demonstrates IC50 values of 0.55 nM, 25.1 nM, and 5.4 nM against TRKWT, TRKG595R, and TRKG667C, respectively. This compound exhibits antiproliferative activity, with IC50 values of 9.5 nM, 3.7 nM, 205.0 nM, and 48.3 nM in various Ba/F3 cell lines expressing ETV6-TRKAWT, ETV6-TRKBWT, LMNA-TRKG595R, and LMNA-TRKAG667C, respectively. TRK-IN-28 is valuable for research focused on TRK-related tumors and signaling pathways. -
TRK Inhibitor
Trk-IN-11 is a highly effective inhibitor of tropomyosin receptor kinase (TRK), exhibiting IC50 values of 1.4 nM and 1.8 nM against TrkA and TrkAG595R, respectively. As a receptor tyrosine kinase, TRK plays a crucial role in the progression of solid tumors. This compound is valuable for studying TRK-related pathways and assessing therapeutic strategies in cancer research. -
TRK Inhibitor
(R)-Larotrectinib is a selective TRK inhibitor, demonstrating an IC50 value of 28.5 nM for TrkA. This compound is instrumental in advancing research on cancers associated with TRK fusions, offering potential insights into therapeutic strategies. Additionally, (R)-Larotrectinib may contribute to the understanding of inflammatory and certain infectious diseases, making it a valuable reagent for diverse biomedical investigations. -
Trk Receptor Inhibitor
Pan-Trk-IN-2 is a small molecule inhibitor targeting the Trk receptor family. It demonstrates potent antitumor activity by interfering with nerve growth factor signaling pathways. This compound is useful for research applications focused on cancer biology and the therapeutic exploration of neurotrophic receptor pathways. -
TrkB Agonist
TrkB-IN-1 is a potent agonist of the tropomyosin receptor kinase B (TrkB), exhibiting favorable pharmacokinetic properties. This compound has demonstrated the ability to reverse cognitive deficits in Alzheimer's disease mouse models, making it a valuable tool for investigating therapeutic strategies in neurodegenerative research. TrkB-IN-1 may facilitate the exploration of synaptic plasticity and neuroprotection, contributing to the understanding of TrkB signaling pathways in Alzheimer's disease. -
Trk Inhibitor
Trk-IN-1 is a potent inhibitor of tropomyosin-related kinases (Trk), demonstrating significant activity against TrkA with an IC50 of 3.7 nM and TrkB with an IC50 of 94 nM. This compound is useful for studying the role of Trk signaling in various biological processes, including neuronal growth and survival. Trk-IN-1 can be applied in drug discovery efforts aimed at treating conditions associated with Trk dysregulation, such as certain neurodegenerative diseases and cancers. -
TrkA Inhibitor
TrkA-IN-7 is a selective inhibitor of Tropomyosin Receptor Kinase A (TrkA), exhibiting a Kd value of 40 μM. This compound serves as a valuable tool for investigating the role of TrkA in various biological processes, including neurotrophic signaling and cancer progression. Its application in research facilitates the exploration of therapeutic strategies targeting TrkA-related pathways. -
TRK Inhibitor
Trk-IN-10 is a selective inhibitor of tropomyosin receptor kinases (TRK) with IC50 values of 0.86 nM for TrkA and 6.92 nM for the TrkAG595R variant. As a receptor tyrosine kinase, TRK plays a crucial role in the development of solid tumors. Trk-IN-10 exhibits a noteworthy selectivity profile, showing an IC50 of 350 nM against ALK, which may help mitigate potential off-target effects and toxicity in therapeutic applications. This compound is valuable for research into TRK-related pathways and the treatment of neurotrophic receptor-driven malignancies. -
Trk Receptor Inhibitor
Trk-IN-6 is a selective inhibitor of Trk receptors, demonstrating remarkable in vitro potency against various TRK mutants with IC50 values ranging from 0.2 to 0.7 nM. This compound is invaluable for studying the role of Trk signaling in cancer and neurodevelopmental disorders. Its high specificity makes it a reliable tool for elucidating the biological effects of Trk inhibition in research applications. -
TRK Mutant Kinase Inhibitor
TRK-IN-34 is a potent TRK and TRKC mutant kinase inhibitor, exhibiting IC50 values of 0.75 nM and 0.96 nM against TRKAG595R and TRKAG667C, respectively. This compound effectively inhibits the kinase activities of these mutations, leading to decreased proliferation of TRKA-transfected cells and demonstrating tumor growth-inhibitory effects in xenograft models. TRK-IN-34 is valuable for investigating cancers resistant to TRK inhibitors, particularly those driven by the TRKAG667C mutation. -
TrkC Inhibitor
TrkC-IN-1 is a selective inhibitor of Tropomyosin receptor kinase C (TrkC), exhibiting IC50 values of 3.3-7.1 μM in EBC-1 cells and 7.3-10.2 μM in HT-29 cells. This compound demonstrates significant potential in cancer research, particularly in elucidating the role of TrkC in oncogenic signaling pathways. TrkC-IN-1 is a valuable tool for studying the therapeutic implications of targeting TrkC in various cancer types. -
TRK Inhibitor
Type II TRK inhibitor 1 is a selective inhibitor targeting TRK fusion proteins and wild-type TRK, demonstrating potent anti-proliferative effects in Ba/F3 cell lines that express the CD74-TRKAG667C and ETV6-TRKCG696C variants, with IC50 values of 6 nM and 1.7 nM, respectively. Additionally, this compound functions as a click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling its application in bioconjugation and related chemical biology research. -
TrkA Inhibitor
D5261 is a potent allosteric inhibitor of tropomyosin-related kinase A (TrkA). It selectively targets the type III binding site, effectively modulating TrkA activity. D5261 has shown promise in biological assays for studying neuronal development and neurodegenerative diseases, making it a valuable tool for research focused on neurobiology and related therapeutic applications. -
TrkA Kinase Inhibitor
Anizatrectinib is a highly potent and orally bioavailable TrkA kinase inhibitor with an IC50 value of 1.3 nM. This compound plays an important role in the investigation of inflammatory diseases, including prostatitis and other pelvic conditions. Its mechanism of action offers valuable insights into cellular signaling pathways associated with pain and inflammation, making it a useful tool for researchers in the field of therapeutic development. -
TRKA Inhibitor
NMS-P626 is a potent inhibitor of the tropomyosin receptor kinase A (TRKA), TRKB, and TRKC, demonstrating IC50 values of 8 nM, 7 nM, and 3 nM, respectively. This compound effectively inhibits the proliferation of KM12 colorectal cancer cells by suppressing the phosphorylation of TPM3-TRKA and disrupting downstream signaling pathways, with an observed IC50 of 19 nM in these cells. NMS-P626 is valuable for research applications focused on colorectal cancer and related signaling mechanisms. -
TRK Kinase Inhibitor
(3aR)-Selitrectinib is a potent TRK kinase inhibitor, demonstrating IC50 values of 0.6 nM for TRKA and less than 2.5 nM for TRKC. This next-generation compound is designed to target TRK signaling pathways, making it a valuable tool in cancer research. Its selective inhibition of TRK kinases can aid in the investigation of tumorigenesis and the therapeutic potential in TRK fusion-positive cancers.
