Catalog No.
Product Name
Application
Product Information
Citations
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p210Bcr-Abl Kinase Inhibitor
PD180970 is a potent ATP-competitive inhibitor of the p210Bcr-Abl kinase, exhibiting an IC50 of 5 nM for the inhibition of its autophosphorylation. Additionally, it inhibits Src and KIT kinases with IC50 values of 0.8 nM and 50 nM, respectively. PD180970 effectively induces apoptosis in K562 leukemic cells, making it a valuable reagent for research on chronic myelogenous leukemia. -
ALKBH5 Inhibitor
W23-1006 is a selective and covalent inhibitor of ALKBH5, targeting the C200 residue with an IC50 of 3.848 μM. This compound exhibits approximately 30-fold and 8-fold greater inhibitory activity against ALKBH5 compared to FTO and ALKBH3, respectively. W23-1006 is particularly valuable for research applications focusing on triple-negative breast cancer (TNBC), enabling studies on the role of ALKBH5 in tumor biology and potential therapeutic strategies. -
FAK Inhibitor
YH-306 is a selective FAK (Focal Adhesion Kinase) inhibitor that exhibits potent antitumor activity. It effectively suppresses colorectal tumor growth and metastasis by inhibiting key signaling pathways, leading to significant reductions in the migration and invasion of colorectal cancer cells. YH-306 also induces apoptosis and inhibits the proliferation of cancer cells by disrupting the activation of FAK, c-Src, paxillin, and downstream effectors such as PI3K and Rac1, while downregulating MMP2 and MMP9 expression. Additionally, this compound impedes actin polymerization mediated by the Arp2/3 complex, contributing to its antitumor effects. -
FAK Inhibitor
GSK-2256098 hydrochloride is a selective inhibitor of focal adhesion kinase (FAK), known for its antiangiogenic and antineoplastic properties. By targeting FAK, it effectively disrupts tumor cell growth through the modulation of key cellular processes, including adhesion, migration, proliferation, and survival. This compound is valuable for researchers investigating the mechanisms of cancer progression and the development of potential therapeutic strategies. -
EGFR Inhibitor
EGFR-IN-86 is a potent EGFR inhibitor, exhibiting an IC50 of 1.5 nM. It demonstrates significant biological activity against glioblastoma by inducing apoptosis and causing cell cycle arrest in the G2/M phase in U87 cells. This compound serves as a valuable tool for research focused on targeting EGFR in cancer therapy. -
p210bcr/abl Inhibitor
Adaphostin, a potent inhibitor of the p210bcr/abl fusion protein (IC50 = 14 μM), exhibits significant anti-leukemic activity. It induces apoptosis in T-lymphoblastic leukemia cell lines, with IC50 values ranging from 17 to 216 nM. This compound demonstrates selective efficacy against both chronic and acute myeloid leukemia cells and increases reactive oxygen species (ROS) levels in chronic lymphocytic leukemia (CLL) B cells, making it valuable for research in leukemia therapeutics and cellular pathways related to oxidative stress. -
Bcr-Abl Inhibitor
HG-7-85-01 is a type II ATP competitive inhibitor that targets Bcr-Abl, including its T315I mutant, as well as PDGFRα, Kit, and Src kinases. It demonstrates potent inhibition with IC50 values of 3 nM for T315I Bcr-Abl, 20 nM for KDR, and 30 nM for RET, while showing minimal activity against other kinases (IC50 > 2 μM). HG-7-85-01 effectively inhibits cell proliferation through the induction of apoptosis and the suppression of cell-cycle progression, making it a valuable tool for research in cancer biology. -
FGFR2 ADC
Aprutumab ixadotin is an antibody-drug conjugate (ADC) that targets fibroblast growth factor receptor 2 (FGFR2). It combines a fully human anti-FGFR2 monoclonal antibody with an innovative non-cleavable linker conjugated to an Auristatin W derivative. This reagent is primarily utilized in research focused on advanced solid tumors, including FGFR2-positive gastric cancer and triple-negative breast cancer, facilitating the exploration of targeted therapies in these malignancies. -
Syk Inhibitor
PRT062607 acetate is a potent Syk inhibitor with an IC50 of 1 nM, designed for oral administration. This compound effectively inhibits inflammatory pathways and induces apoptosis, demonstrating significant antitumor activity in tumor xenograft mouse models. It serves as a valuable tool in cancer research and the study of Syk-mediated signaling. -
FAK Inhibitor
FAK-IN-2 is a potent inhibitor of focal adhesion kinase (FAK), exhibiting a reported IC50 of 35 nM. This compound effectively covalently modifies and inhibits the autophosphorylation of FAK, leading to significant inhibition of tumor cell migration and clonal formation. Additionally, FAK-IN-2 induces apoptosis in cancer cells, highlighting its potential utility in oncological research and therapeutic applications targeting FAK signaling pathways. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3, exhibiting IC50 values of 13 nM, 73 nM, and 56 nM, respectively. This orally active compound demonstrates significant efficacy in inhibiting the proliferation of various cancer cell lines. It is a valuable tool for research into therapeutic strategies targeting cell cycle regulation and signal transduction pathways in cancer. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib citrate is a potent inhibitor targeting CDK2, JAK2, and FLT3 kinases. This compound demonstrates significant biological activity in disrupting cell cycle progression and signaling pathways associated with cell proliferation and survival. It is utilized in cancer research applications, particularly for studies involving hematological malignancies and solid tumors where these kinases are dysregulated. -
Btk Inhibitor
LFM-A13 is a selective Bruton's tyrosine kinase (BTK) inhibitor known for its capacity to inhibit JAK2 and PLK. With IC50 values of 2.5 μM for recombinant BTK, 10 μM for JAK2, and 61 μM for PLK3, LFM-A13 exhibits significant antiproliferative and anticancer properties. This compound is valuable for research applications focused on cancer biology and therapeutic interventions targeting BTK and related signaling pathways. -
SYK Inhibitor
GSK2646264 is a potent and selective inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC50 value of 7.1. This compound also shows inhibitory activity against several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, and Aurora kinases, with varying pIC50 values. Due to its ability to penetrate the epidermis and dermis, GSK2646264 is potentially valuable for research applications in dermatological conditions and immune responses. -
JAK2/FLT3 Inhibitor
Pacritinib hydrochloride is a selective inhibitor targeting JAK2 and FLT3, demonstrating inhibitory potency against wild-type JAK2 (IC50=23 nM), the JAK2V617F mutant (IC50=19 nM), and FLT3 (IC50=22 nM) as well as the FLT3D835Y mutant (IC50=6 nM). This compound is primarily utilized in research related to acute myeloid leukemia (AML) and myelofibrosis (MF), making it a valuable tool for studying these hematological malignancies and the associated signaling pathways. -
SYK/JAK Inhibitor
Gusacitinib hydrochloride is a potent dual inhibitor of SYK and JAK kinases, demonstrating IC50 values of 5 nM, 46 nM, 4 nM, 11 nM, and 8 nM for SYK, JAK1, JAK2, JAK3, and TYK2, respectively. This compound effectively suppresses critical inflammatory pathways linked to the pathogenesis of atopic dermatitis. Gusacitinib hydrochloride is suitable for research applications involving chronic hand eczema and various cancers, including basal cell carcinoma. -
PROTAC FLT3/JAK2/BRD4 Degrader
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML). -
JAK3/BTK Inhibitor
JAK3/BTK-IN-3 is a selective inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). Targeting both JAK3 and BTK can provide synergistic effects beneficial for the therapeutic intervention of autoimmune diseases. This compound is suitable for research applications focused on elucidating the roles of JAK3 and BTK in various disease mechanisms, facilitating the development of novel treatment strategies. -
JAK2/FLT3 Inhibitor
SB1578 is a selective inhibitor of JAK2 and FLT3, exhibiting IC50 values of 46 nM and 60 nM, respectively. This compound demonstrates high selectivity for other kinase targets, making it a valuable tool for research. SB1578 is particularly useful in studying non-oncological indications, such as rheumatoid arthritis, offering insights into potential therapeutic applications in inflammatory diseases. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-7 is a potent inhibitor targeting Janus kinase 3 (JAK3) and Bruton’s tyrosine kinase (BTK), demonstrating IC50 values of 2 nM and 14 nM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating the underlying mechanisms of rheumatoid arthritis. Its efficacy in modulating inflammatory pathways highlights its potential in related therapeutic research applications. -
CDK2/JAK2/FLT3 Inhibitor
Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-2 is a potent dual inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). By simultaneously targeting the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that may enhance therapeutic outcomes in autoimmune diseases. JAK3/BTK-IN-2 is suitable for research applications focused on JAK3 and BTK-related pathologies, facilitating studies on their roles in immune regulation and disease progression. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-5 is a potent dual inhibitor targeting Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). This compound effectively disrupts the BTK/JAK3 signaling pathway, demonstrating potential synergistic effects advantageous for the treatment of autoimmune diseases. JAK3/BTK-IN-5 is valuable for research into conditions related to JAK3 kinase and BTK, making it a crucial tool for studying the pathophysiology of these targets. -
FLT3/JAK2/BRD4 Ligand
FLT3/JAK2/BRD4 ligand-1 is a specific ligand for the FLT3, JAK2, and BRD4 proteins. This compound facilitates the design and synthesis of proteolysis-targeting chimeras (PROTACs), specifically PROTAC FLT3/JAK2/BRD4 Degrader-1. It demonstrates potential applications in targeted protein degradation and cancer research, enabling innovative therapeutic strategies against malignancies associated with these targets. -
FLT3 Inhibitor
JI6 is a potent and selective FLT3 inhibitor, exhibiting IC50 values of approximately 40 nM for FLT3-WT, 8 nM for FLT3-D835Y, and 4 nM for FLT3-D835H. Additionally, JI6 demonstrates inhibitory activity against JAK3 and c-Kit, with IC50 values of around 250 nM and 500 nM, respectively. This compound serves as a valuable tool for research applications focused on acute myeloid leukemia. -
BTK/JAK3 Inhibitor
JAK3/BTK-IN-6 is a potent dual inhibitor targeting Bruton's Tyrosine Kinase (BTK) and Janus Kinase 3 (JAK3), exhibiting IC50 values of 0.6 nM and 0.4 nM, respectively. This compound demonstrates excellent metabolic stability in human liver microsomes, making it suitable for in vitro studies. JAK3/BTK-IN-6 is valuable in research applications related to hematological disorders and immune system dysfunctions. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-4 is a potent inhibitor targeting both JAK3 and BTK kinases, which are critical in the modulation of immune responses involved in autoimmune diseases. By simultaneously inhibiting the BTK/JAK3 signaling pathway, JAK3/BTK-IN-4 demonstrates synergistic effects, making it a valuable tool for studying JAK3 and BTK-related pathologies. This compound is particularly relevant for research applications focused on therapeutic strategies for autoimmune disorders. -
SYK/JAK Inhibitor
SYK/JAK-IN-1 is a dual inhibitor targeting SYK and JAK2, exhibiting IC50 values of less than 5 nM for both kinases. This compound demonstrates significant anti-inflammatory and anti-proliferative activities, making it a valuable tool for research involving hematological malignancies and autoimmune disorders. Its potent inhibition profile allows for the exploration of signaling pathways associated with SYK and JAK2, facilitating studies in cancer biology and immunology. -
BET/JAK2/FLT3 Inhibitor
SG3-179 is a selective inhibitor of BET bromodomain proteins, with additional activity against JAK2 and FLT3. This compound effectively reduces HOXB13 protein expression, demonstrating potential relevance in the study of multiple myeloma (MM1.S). SG3-179 is a valuable tool for research involving epigenetic regulation and signaling pathways associated with hematological malignancies. -
JAK3/BTK Inhibitor
JAK3/BTK-IN-1 is a potent dual inhibitor targeting JAK3 and BTK, key proteins implicated in autoimmune diseases. By simultaneously blocking the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that could enhance therapeutic outcomes. JAK3/BTK-IN-1 is suitable for research into JAK3 kinase and BTK-related diseases, facilitating the exploration of innovative treatment strategies in immunology and related fields. -
JAK3/Syk Inhibitor
R-348 choline is a potent, orally active inhibitor of Janus kinase 3 (JAK3) and spleen tyrosine kinase (Syk). This compound effectively reduces the expression levels of pro-inflammatory cytokines, including interferon-gamma (IFN-γ), interleukin-6 (IL-6), and interleukin-10 (IL-10). R-348 choline is primarily utilized in research related to acute cardiac allograft rejection and other autoimmune conditions where JAK3 and Syk signaling play critical roles. -
FGFR1 Agonist
TCB-32 is a potent FGFR1 agonist with an EC50 of 0.88 μM, effectively activating the FGFR1 signaling pathway to enhance cell proliferation, notably through the ERK 1/2 cascade. This compound exhibits excellent thermal stability and can serve as a substitute for bFGF in serum-free cell culture environments. TCB-32 is applicable in research related to tissue repair and wound healing, making it suitable for studies investigating conditions such as psoriasis and eczema. -
FGFR3/BRAF Binder
2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose functions as a selective binder for Fibroblast Growth Factor Receptor 3 (FGFR3) and BRAF, playing a pivotal role in modulating pathways associated with cancer progression. Derived from Atractylodes japonica, this compound exhibits low cytotoxicity towards cancer cell lines, making it a suitable candidate for research applications focused on targeted cancer therapies and signaling pathway studies. Its unique structural characteristics enhance its potential for further exploration in drug development and therapeutic interventions. -
bFGF/FGFR1 Ligand
bFGF (119-126) is a peptide ligand that selectively targets FGFR1, disrupting the bFGF-FGFR1 interaction, which leads to inhibition of FGFR1 phosphorylation and subsequent downstream signaling pathways. This results in the promotion of apoptosis and suppression of cell proliferation, migration, angiogenesis, and metastasis. Additionally, when conjugated with a carrier, bFGF (119-126) enhances cellular uptake through FGFR-mediated endocytosis, serving as an effective FGFR-targeting agent. Its applications extend to research in various cancers, including lung cancer, breast cancer, glioblastoma, and ovarian cancer, particularly when combined with ultrasound and Doxorubicin to potentiate antitumor effects. -
FGFR3 Inhibitor
Dabogratinib is a selective inhibitor of FGFR3, displaying an IC50 of 11 nM. It demonstrates significant antitumor activity against urothelial carcinoma and various solid tumors by downregulating FGFR3 and ERK1/2 signaling pathways, leading to tumor growth inhibition and regression in FGFR3-altered xenograft models. Additionally, Dabogratinib enhances chondrocyte proliferation and differentiation, promotes endochondral bone formation, and improves craniofacial and spinal morphology. This compound is valuable for research into metastatic urothelial carcinoma, achondroplasia, and hypochondroplasia. -
FGFR2 Inhibitor
FGFR2-IN-2 is a selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), demonstrating inhibitory potency with an IC50 value of 29 nM against FGFR2, and 389 nM and 758 nM for FGFR1 and FGFR3, respectively. This compound exhibits potential in the study of FGFR-related signaling pathways and can be utilized in research focused on cancer therapeutics, particularly in tumors with aberrant FGFR2 activity. -
FGFR Inhibitor
FIIN-1 is a selective, irreversible inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2, FGFR3, and FGFR4). It exhibits potent binding affinity, with Kd values of 2.8 nM for FGFR1, 6.9 nM for FGFR2, 5.4 nM for FGFR3, and 120 nM for FGFR4, alongside Kd values of 32 nM and 120 nM for Flt1 and Flt4, respectively. With biochemical IC50 values of 9.2 nM for FGFR1, 6.2 nM for FGFR2, 11.9 nM for FGFR3, and 189 nM for FGFR4, FIIN-1 is valuable for research applications focused on FGFR-related pathways in cancer and developmental biology. -
FGFR-β-klotho complex Activator
Efimosfermin alfa is a genetically modified variant of FGF21 that activates the FGFR1c/β-Klotho complex. This compound plays a critical role in metabolic regulation, specifically in the context of metabolic dysfunction-associated steatohepatitis, obesity, and mild hypertriglyceridemia. Its unique mechanism of action makes it a valuable tool for research exploring metabolic disorders and their associated pathways. -
FGFR1 Inhibitor
FGFR1 inhibitor-10 is a potent FGFR1 inhibitor with an IC50 value of 28 nM. It effectively inhibits the phosphorylation of FGFR1, leading to significant anti-angiogenic, anti-invasive, and anti-tumor activities. This compound is valuable for research applications focused on understanding FGFR1 signaling pathways and developing therapies for cancers characterized by aberrant FGFR1 activity. -
FGFR3 Inhibitor
FGFR3-IN-5 is a potent and selective inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3), exhibiting IC50 values of 3 nM for FGFR3, 44 nM for FGFR2, and 289 nM for FGFR1. This compound demonstrates effective inhibition of FGFR3 signaling pathways, making it a valuable tool for cancer research. FGFR3-IN-5 is suitable for studies investigating the role of FGFR3 in tumorigenesis and therapeutic response. -
FLT3/FGFR Inhibitor
MAX-40279 is a dual inhibitor targeting FLT3 and FGFR kinases, exhibiting potent activity against both wild-type and FLT3 mutants, including FLT3D835Y. This compound effectively inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 is valuable for research applications in acute myelogenous leukemia (AML), particularly in studying resistance mechanisms to existing therapies. -
FGFR (1-3) Inhibitor
CPL304110 is a selective inhibitor of fibroblast growth factor receptors FGFR1-3, demonstrating potent activity with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for each receptor, respectively. This orally active compound is valuable in research applications aimed at understanding FGFR signaling pathways and their role in various cancers and pathological conditions. Its efficacy in modulating FGFR activity makes it a valuable tool for investigating therapeutic strategies targeting fibroblast growth factor receptor-mediated processes. -
FGFR2 Inhibitor
Lirafugratinib hydrochloride is an orally active, irreversible inhibitor specifically targeting FGFR2 with an IC50 of 3 nM. It covalently binds to the cysteine residue Cys491, effectively addressing FGFR2 primary alterations and resistance mutations. This compound is designed to induce tumor regression while exhibiting minimal impact on other FGFR family members, making it valuable for research in cancer therapeutics focused on FGFR-dependent malignancies. -
FGFR3-TACC3 Degrader
SNIPER(TACC3)-11 is a potent degrader of the FGFR3-TACC3 fusion protein, utilizing targeted protein degradation to reduce its levels within cells. This compound effectively suppresses the proliferation of cancer cells that express the FGFR3-TACC3 fusion, making it a valuable tool for research related to targeting oncogenic protein fusions in cancer therapy. Its potential applications include studies in cancer biology and the development of novel therapeutic strategies against FGFR3-TACC3-positive tumors. -
FGFR Inhibitor
FGFR2-IN-1 is a selective inhibitor of Fibroblast Growth Factor Receptor 2 (FGFR2), exhibiting an IC50 of 140 nM. This compound effectively modulates FGFR2 activity, demonstrating significant biological activity relevant to cancer research. It is utilized in various studies focusing on tumorigenesis and the role of FGFR signaling pathways in malignancies. -
PDGFR Inhibitor
(Z)-Orantinib is a selective, orally active ATP-competitive inhibitor targeting PDGFRβ, as well as Flk‐1/KDR and FGFR1, with IC50 values of 0.008 µM, 2.1 µM, and 1.2 µM, respectively. This compound exhibits significant antiangiogenic and antitumor properties, effectively inducing regression of established tumors. It is a valuable tool for research applications focused on cancer biology and the mechanisms of angiogenesis. -
FGFR4 Inhibitor
FGFR4-IN-5 is a selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 of 6.5 nM. It demonstrates significant anti-tumor activity in vivo, making it a valuable tool for research focused on hepatocellular carcinoma. This compound is ideal for studies investigating FGFR4-mediated signaling pathways and therapeutic strategies in cancer treatment. -
FGFR1 Inhibitor
CYY292 is an FGFR1 inhibitor that targets the FGFR1/AKT/Snail signaling pathway, demonstrating significant effects in glioblastoma (GBM) cells. This compound effectively inhibits cancer cell proliferation and reduces epithelial-mesenchymal transition, stemness, invasion, and migration in a dose-dependent manner. CYY292 is a valuable reagent for research applications aimed at understanding the molecular underpinnings of GBM and exploring potential therapeutic strategies. -
FGFR2 Inhibitor
FGFR2-IN-3 is a selective inhibitor of fibroblast growth factor receptor 2 (FGFR2). It exhibits strong binding affinity, facilitating critical interactions and inducing conformational alterations in the receptor. This compound is primarily utilized in cancer research, particularly in investigations focused on tumor biology and signaling pathways involving FGFR2. -
VEGFR2 Inhibitor
JK-P3 is a selective inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) with IC50 values of 7.83 μM for VEGFR2, 27 μM for FGFR1, and 5.18 μM for FGFR3. It effectively blocks VEGF-A-induced VEGFR2 activation and downstream signaling pathways, demonstrating inhibition of endothelial cell migration and angiogenesis in vitro. Additionally, JK-P3 suppresses fibroblast growth factor receptor kinase activity, contributing to its anti-angiogenic properties and making it a valuable tool for research in vascular biology and cancer therapeutics.
