Catalog No.
Product Name
Application
Product Information
Citations
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Ligands for Target Protein for PROTAC
PROTAC IRAK4 ligand-1 is a synthetic ligand specifically designed to target interleukin-1 receptor-associated kinase 4 (IRAK4). This compound plays a critical role in the development of PROTAC IRAK4 degrader-1, facilitating targeted protein degradation. Its primary applications include cancer research and studies investigating inflammatory pathways, making it a valuable tool for researchers exploring IRAK4-related signaling mechanisms. -
PROTAC Ligand
PROTAC IRAK4 ligand-3 is a PROTAC ligand that selectively targets IRAK4, an integral component of the Toll-like receptor signaling pathway. This compound facilitates the targeted degradation of IRAK4, thereby influencing key signaling cascades involved in inflammation and cancer. It is valuable for research applications focusing on cancer therapies and the modulation of inflammatory responses. -
Ligands for Target Protein for PROTACs
IRAK4 ligand-12 is a ligand for interleukin-1 receptor-associated kinase 4 (IRAK4), designed for use in PROTAC (proteolysis targeting chimeras) applications. This compound plays a critical role in the selective degradation of IRAK4, thus enabling the modulation of immune response pathways. It is particularly useful in research focused on inflammation and cancer, facilitating studies on targeted protein degradation strategies. IRAK4 ligand-12 can also be utilized in the synthesis of KTX-951, contributing to advancements in therapeutic development. -
Ligand for Target Protein for PROTAC
PROTAC IRAK4 ligand-5 is a ligand designed for use in proteolysis targeting chimera (PROTAC) applications, specifically targeting IRAK4. This compound plays a crucial role in the synthesis of KT-413, facilitating the degradation of IRAK4 to modulate immune responses. It is of particular interest for research in inflammatory diseases and therapeutic development involving targeted protein degradation. -
E3 ligase ligand
E3 ligase Ligand 38 functions as an E3 ligase ligand, facilitating the development of targeted protein degraders. It is notably utilized in the synthesis of PROTAC IRAK4 degrader-12, contributing to innovative strategies in degrading specific proteins. This compound is essential for research applications focused on protein homeostasis and the modulation of intracellular signaling pathways. -
Intermediate
Thalidomide-NH-C2-azaspiro[3.5]nonane hydrochloride serves as a crucial intermediate in the synthesis of IRAK degraders. Its structural properties facilitate the development of compounds that modulate immune responses by targeting IRAK proteins. This reagent is valuable for researchers focusing on therapeutic applications in inflammatory diseases and immune regulation. -
E3 Ligase Ligand-linker Conjugate
E3 Ligase Ligand-linker Conjugate 226 is a synthetic conjugate utilized in the development of PROTACs targeting E3 ligases. This compound facilitates the synthesis of PROTAC IRAK3 degrader-2, possessing significant anti-tumor activity. It serves as a key tool in research applications focused on targeted protein degradation and therapeutic strategies for oncological diseases. -
E3 Ligand-Linker Conjugate
CRBN Ligand-Linker Conjugate 2 is an E3 ligand-linker conjugate designed for the synthesis of proteolysis-targeting chimeras (PROTACs). This compound facilitates targeted degradation of specific proteins by harnessing the ubiquitin-proteasome system. It has been utilized in the development of FIP22, a highly selective IRAK4 PROTAC degrader, which demonstrates potential therapeutic activity against atopic dermatitis. Researchers can leverage this conjugate for advancements in targeted protein degradation strategies. -
E3 Ligase Ligand-linker Conjugate
E3 Ligase Ligand-linker Conjugate 125 is a specialized conjugate designed to engage E3 ligases for targeted protein degradation. This reagent facilitates the synthesis of PROTAC IRAK4 degrader-12, enabling selective degradation of IRAK4, which is implicated in various signaling pathways and inflammatory processes. It serves as a valuable tool in chemical biology and therapeutic research, particularly in the study of targeted protein modulation and novel drug development strategies. -
TrkA-NGF Interaction Inhibitor
TrkA/NGF-IN-1 is a potent inhibitor of the interaction between TrkA and nerve growth factor (NGF), with an IC50 of 21 nM as determined by the PathHunter assay. This peptide demonstrates significant analgesic activity in rodent models of incisional pain, making it a valuable tool for research on pain mechanisms and therapeutic interventions targeting the TrkA signaling pathway. -
Trk Kinase Inhibitor
Trk-IN-2 is a potent pan-Trk kinase inhibitor, demonstrating an IC50 of 9 nM for the TrkA enzyme and a cell-based IC50 of 7 nM. This compound exhibits significant pharmacodynamic effects in rat models of inflammatory and neuropathic pain. Trk-IN-2 is valuable for research applications focused on the mechanisms and treatment of inflammatory pain and neuropathic pain conditions. -
ErbB-2/EGFR Tyrosine Kinase Inhibitor
GW583340 is an orally bioavailable inhibitor targeting the ErbB-2 and EGFR tyrosine kinases. It demonstrates significant antitumor activity in xenograft models characterized by overexpression of EGFR or ErbB-2, making it a valuable tool for investigating therapeutic strategies. GW583340 is particularly relevant for research focused on head and neck cancer, breast cancer, and gastric cancer. -
ALK Inhibitor
TSR-011-isomer is a potent anaplastic lymphoma kinase (ALK) inhibitor with an IC50 of 6 nM. This compound demonstrates significant biological activity by undergoing metabolic hydrolysis and NADPH-dependent metabolism, facilitating its clearance in biological systems. TSR-011-isomer is suitable for research focused on ALK-driven cancers, making it a valuable tool for studies in cancer biology and targeted therapy development. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
TIE2/STK10/BRK Inhibitor
SB-633825 is a potent ATP-competitive inhibitor targeting TIE2, LOK (STK10), and BRK, with IC50 values of 3.5 nM, 66 nM, and 150 nM, respectively. This compound effectively inhibits cancer cell proliferation and angiogenesis, making it a valuable tool for research on tumor growth and vascular development. Its selective inhibition profile supports studies aimed at understanding the roles of these kinases in cancer biology and therapeutic strategies. -
EGFR PARP Dual-targeting PROTAC Molecule
DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies. -
PROTAC Linkers
AM-Imidazole-PA-Boc is a versatile PROTAC linker characterized by its alkyl chain structure. It plays a critical role in the design and synthesis of PROTAC IRAK4 degrader-1, facilitating targeted protein degradation. This compound is essential for researchers exploring the therapeutic potential of targeted protein degradation in various signaling pathways and disease models. -
ITK Degrader
ITK Degrader 2 is a PROTAC-based compound that specifically targets and degrades the interleukin-2-inducible T-cell kinase (ITK) with a DC50 value of less than 10 nM. In pharmacokinetic studies in mice, this orally active degrader demonstrates a maximum concentration (Cmax) of 0.87 μM and achieves peak plasma levels (Tmax) at 2 hours post-administration. At a dosage of 90 mg/kg, ITK Degrader 2 effectively reduces ITK levels by 20% within 6 hours, making it a valuable tool for exploring ITK-related signaling pathways and their implications in immune responses. -
SRC-1 Degrader/PROTAC
ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis. -
EGFR T790M/L858R/ACK1 Inhibitor
EGFR/ACK1-IN-1 is a potent inhibitor targeting the EGFR T790M/L858R mutation and ACK1, with IC50 values of 23 nM and 263 nM, respectively. This dual inhibition effectively disrupts cell proliferation and demonstrates significant antitumor activity. It is a valuable reagent for research applications focused on cancer biology and therapeutic development for EGFR mutant-driven tumors. -
Ack1 Inhibitor
Ack1 inhibitor 2 is a selective inhibitor of the Ack1 kinase, demonstrating an IC50 value of 0.46 μM. This compound effectively modulates the Ack1 signaling pathway, which plays a critical role in various cellular processes, including cell proliferation and survival. Ack1 inhibitor 2 is primarily utilized in research applications focused on cancer biology and molecular signaling studies. -
ALK Degrader
ALK-IN-35 is an ALK degrader that selectively inhibits ALK kinase activity with an IC50 of 0.74 nM. This compound increases the solvent-accessible surface area of hydrophobic residues around the ALK binding pocket, leading to a partially unfolded conformation that promotes proteasomal degradation of ALK. ALK-IN-35 has demonstrated potent anti-proliferative effects on cancer cells and is a valuable tool for research focused on non-small cell lung cancer. -
ALK Inhibitor
XMU-MP-5 is a selective inhibitor of anaplastic lymphoma kinase (ALK), demonstrating potent inhibitory activity against ALK-mutated Ba/F3 cells with IC50 values ranging from 4 to 50 nM. This compound induces apoptosis specifically in EML4-ALK Ba/F3 cells and has shown notable antitumor efficacy in murine models. XMU-MP-5 serves as a valuable tool in cancer research, particularly in studies focused on ALK-driven malignancies. -
ALK Inhibitor
Ceritinib mesylate is a selective ALK tyrosine kinase inhibitor that functions through ATP-competitive mechanisms, exhibiting an IC50 of 200 pM. In addition to its activity against ALK, Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D, with IC50 values of 8 nM, 7 nM, and 23 nM, respectively. This compound demonstrates significant antitumor potency, making it a valuable tool for research in cancer biology and targeted therapies. -
DDR Inhibitor
7rh is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 13.1 nM, and also demonstrates moderate inhibitory activity against DDR2 with an IC50 of 203 nM. This compound serves as a valuable tool for the study of receptor signaling and cellular processes associated with DDRs. Additionally, 7rh incorporates an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it suitable for applications in click chemistry. -
DDR1 DDR2 FLT1 Inhibitor
TPKI-39 is an inhibitor of DDR1, DDR2, and FLT1, demonstrating a human DDR1 IC50 of 380 nM and human DDR2 IC50 of 120 nM. It effectively inhibits enzymatic activity and autophosphorylation of DDR1 and DDR2, as well as FLT1 enzymatic activity, with an IC50 of 65 nM. This compound is useful for studies focused on the modulation of receptor tyrosine kinases and collagen-mediated signaling pathways. -
TIE2 Inhibitor
BAY-826 is a selective and potent inhibitor of the TIE2 receptor, exhibiting a binding affinity (Kd) of 1.6 nM. This compound plays a significant role in studying angiogenesis and vascular biology by modulating TIE2 signaling pathways. Its application in research encompasses tumor microenvironment studies, vascular disorder investigations, and potential therapeutic strategies targeting vascular-related diseases. -
DDR1/2 Inhibitor
VU6015929 is a potent and selective dual inhibitor of discoidin domain receptors 1 and 2 (DDR1/2), exhibiting IC50 values of 4.67 nM and 7.39 nM, respectively. This compound effectively inhibits collagen-induced activation of DDR1 and reduces collagen-IV production, making it a valuable tool for research on fibrosis and extracellular matrix remodeling. VU6015929 is suitable for studying the roles of DDR1/2 in various pathological processes and therapeutic interventions. -
Discoidin Domain Receptor Inhibitor
DDR1-IN-4 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), effectively blocking its autophosphorylation with an IC50 of 29 nM. This compound exhibits significantly lower activity against DDR2, with an IC50 of 1.9 μM. DDR1-IN-4 is utilized in research applications focusing on cell signaling, extracellular matrix interactions, and cancer biology, providing valuable insights into the role of DDR1 in various pathological conditions. -
DDR2 Inhibitor
DDR2-IN-1 is a potent inhibitor of the Discoidin Domain Receptor 2 (DDR2) with an IC50 of 26 nM. This compound plays a significant role in research related to osteoarthritis by modulating collagen signaling pathways and potentially influencing cartilage degradation and repair. Its application in studying DDR2-mediated processes makes it a valuable tool for investigating therapeutic strategies in bone and joint diseases. -
DDR1 Inhibitor
DDR1-IN-6 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), exhibiting an IC50 of 9.72 nM. This compound effectively inhibits auto-phosphorylation at the Y513 site of DDR1b, also with an IC50 of 9.7 nM, demonstrating significant anti-cancer activity. Additionally, DDR1-IN-6 serves as a click chemistry reagent due to its alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, facilitating diverse research applications in chemical biology and drug discovery. -
Discoidin Domain Receptor Inhibitor
DDR Inhibitor is a highly selective inhibitor of the discoidin domain receptors (DDRs), specifically demonstrating an IC50 of 3.3 nM for DDR2. Additionally, it exhibits a significant inhibitory effect on DDR1, with 53% inhibition at a concentration of 1.5 nM. This compound is valuable for investigating the role of DDRs in cellular processes and may have applications in cancer research and fibrosis studies. -
DDR1/DDR2 Inhibitor
DDR1/2 inhibitor-2 is a selective inhibitor of the DDR1 and DDR2 receptor tyrosine kinases, demonstrating IC50 values of less than 100 nM. This compound is primarily utilized in research related to cancer and fibrotic diseases, providing insights into the role of these receptors in tumor progression and fibrosis. Its potent inhibitory effects make it a valuable tool for studying DDR signaling pathways and their contributions to disease mechanisms. -
DDR1 Inhibitor
DDR1-IN-5 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), demonstrating an IC50 of 7.36 nM. It effectively inhibits the auto-phosphorylation of DDR1b at Y513, with an IC50 of 4.1 nM. DDR1-IN-5 exhibits anti-cancer activity, making it a valuable tool for cancer research. Additionally, this compound features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition for further biochemical applications. -
Discoidin Domain Receptor Inhibitor
DDR1-IN-9 is a selective inhibitor of the Discoidin Domain Receptor 1 (DDR1), known for its significant suppression of kinase activity, with a Kd value of 4.7 nM and an IC50 value of 9.4 nM. Demonstrating reduced activity against a broad panel of 400 nonmutated kinases, DDR1-IN-9 exhibits a favorable specificity profile. This compound also possesses beneficial pharmacokinetic properties and has displayed potential therapeutic effects in experimental models of pulmonary fibrosis, making it a valuable tool for researching fibrotic diseases and DDR1-related signaling pathways. -
DDR1 Inhibitor
DDR1-IN-10 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1). It exhibits significant potential in the modulation of DDR1-mediated signaling pathways, making it a valuable tool in cancer research. DDR1-IN-10 is particularly useful for studying various malignancies, including pancreatic cancer, non-small cell lung cancer, and gastric carcinoma, where DDR1 plays a critical role in tumor progression and metastasis. -
DDR1/2 Inhibitor
DDR1/2 IN-4 is a selective dual inhibitor targeting DDR1 and DDR2 kinases, demonstrating a pKi of 8.6 for DDR1 and 8.2 for DDR2. This compound effectively inhibits the kinase activities of both DDR1 and DDR2, leading to a reduction in the release of MCP-1. DDR1/2 IN-4 is suitable for research applications focused on idiopathic pulmonary fibrosis and related cellular mechanisms. -
DDR1 Inhibitor
DDR1-IN-12 is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 0.126 μM. This compound effectively blocks receptor tyrosine kinase autophosphorylation, thereby inhibiting downstream signaling pathways, including the suppression of TGF-β1-induced fibroblast activation. DDR1-IN-12 demonstrates significant potential in research applications related to tumor cell migration and the progression of pulmonary fibrosis, making it particularly relevant for studies involving lung cancer, including lung adenocarcinoma. -
DDR1/2 Inhibitor
DDR1-IN-8 is a potent dual inhibitor of DDR1 and DDR2, demonstrating IC50 values of 0.045 μM and 0.126 μM, respectively. This compound exhibits significant anti-tumor activity, making it a valuable tool for studies related to cancer research. DDR1-IN-8 can be utilized to explore the role of DDR signaling in tumor progression and therapeutics targeting the DDR pathway. -
DDR1/2 Inhibitor
DDR1/2 inhibitor-3 is a selective inhibitor of discoidin domain receptor 1 and 2 (DDR1/2), exhibiting IC50 values of 9.4 nM and 20.4 nM, respectively. This compound is primarily utilized in anti-inflammatory research, targeting the DDR pathways involved in cellular responses to inflammation. Its potent inhibitory effects make it a valuable tool for elucidating the role of DDR receptors in various biological processes. -
EphB2 Inhibitor
ALW-II-49-7 is a selective inhibitor of the EphB2 kinase, exhibiting an EC50 value of 40 nM in cellular assays. It is designed to effectively disrupt EphB2 signaling pathways, which are implicated in various biological processes including cell adhesion and migration. This reagent is valuable for research applications focusing on cancer biology, neurodevelopment, and the modulation of angiogenesis. -
EphA3 Inhibitor
AWL-II-38.3 is a selective inhibitor of the ephrin-A receptor (EphA3) kinase. This compound demonstrates potent inhibitory activity specifically targeting EphA3 while displaying minimal effects on Src-family kinases and b-raf. Its specificity makes AWL-II-38.3 valuable for research applications involving EphA3-mediated signaling pathways and related cellular processes. -
EphB3 Inhibitor
LDN-211904 oxalate is a potent and reversible inhibitor of EphB3, exhibiting an IC50 of 79 nM. This compound demonstrates favorable metabolic stability in mouse liver microsomes, making it suitable for in vitro studies. LDN-211904 oxalate is particularly relevant for research involving STAT3-activated colorectal cancer stemness and may help overcome Cetuximab resistance in colorectal cancer. -
EphA4 Agonist
150D4 is a selective agonist of EphA4, capable of effectively penetrating the blood-brain barrier. This compound exhibits excitatory activity and provides neuroprotective effects, making it a valuable tool for studying various neurological conditions. Its unique properties make 150D4 suitable for research aimed at understanding the role of EphA4 in neurobiology and developing potential therapeutic strategies. -
EphA2 Receptor Agonist
EphA2 Agonist 1 is a selective agonist for the EphA2 receptor, demonstrating high potency in stimulating EphA2 phosphorylation. This compound exhibits significant effectiveness against glioblastoma cells that overexpress the EphA2 receptor, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to activate EphA2 pathways can aid in elucidating the receptor's role in tumorigenesis and potential interventions. -
Eph/ephrin Antagonist
UniPR129 is a potent, orally active antagonist of Eph/ephrin interactions. It effectively inhibits the EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. This compound has demonstrated the ability to inhibit angiogenesis and exhibits both antitumor and neuroprotective properties. UniPR129 is suitable for research applications in cancer and neurological disorders, including colorectal cancer and optic neuropathy. -
Eph Inhibitor
Eph Inhibitor 1 is a potent inhibitor of Eph receptors, targeting the Eph family of receptor tyrosine kinases. It has demonstrated significant biological activity in modulating cellular signaling pathways involved in neural development and synaptic plasticity. This compound holds promise for research applications related to neurological disorders, facilitating insights into therapeutic strategies for conditions linked to Eph receptor dysregulation. -
EPHA2 Inhibitor
EphA2 antagonist 1 is an ephrin type-A receptor 2 (EPHA2) inhibitor designed to modulate the signaling pathways associated with this receptor. It exhibits significant biological activity in disrupting EPHA2-mediated processes, which may have implications in cancer research and metastasis studies. This compound serves as a valuable tool for investigating the role of EPHA2 in various cellular contexts and therapeutic applications. -
EphA2-Targeting Agent
Targefrin is a potent EphA2-targeting agent that functions as an antagonist. It exhibits high affinity for the EphA2 ligand-binding domain, with a dissociation constant of 21 nM and an IC50 value of 10.8 nM. Targefrin induces internalization and degradation of the EphA2 receptor in various pancreatic cancer cell lines, making it a valuable tool for research on cancer biology and therapeutic targeting of EphA2-related pathways. -
EphA2/EphB2 Antagonist
UniPR1447 is a dual antagonist of EphA2 and EphB2, exhibiting an IC50 of 6.6 μM for the inhibition of the EphA2-ephrin-A1 interaction. This compound serves as a valuable tool in research focused on the role of Eph receptors in cellular processes such as angiogenesis, tumor progression, and neural development. Its application in studies targeting EphA2 and EphB2 signaling pathways contributes to understanding their implications in various diseases, making UniPR1447 a relevant reagent for therapeutic exploration.
