Catalog No.
Product Name
Application
Product Information
Citations
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FAK/Aurora Kinase Inhibitor
FAK/Aurora kinase-IN-1 is a dual inhibitor targeting focal adhesion kinase (FAK) and Aurora kinase, exhibiting IC50 values of 6.61 nM and 0.91 nM, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and therapeutic development. Its efficacy in inhibiting both kinases positions it as a promising candidate for further studies in tumor proliferation and treatment strategies. -
FAK Inhibitor
FAK-IN-10 is a potent inhibitor of focal adhesion kinase (FAK) with an IC50 of 76.3 µM. This compound demonstrates significant antitumor activity, particularly against the MCF-7 and A431 cell lines, exhibiting IC50 values of 4.23 µM and 0.78 µM, respectively. FAK-IN-10 is valuable for research focused on cancer therapeutics and the modulation of signaling pathways associated with tumor growth and metastasis. -
ALK/c-Met/ROS1 Inhibitor
Crizotinib acetate is an orally bioavailable inhibitor targeting ALK, c-Met, and ROS1 through ATP competition. It demonstrates potent inhibition of tyrosine phosphorylation in cell-based assays, with IC50 values of 20 nM for ALK, 8 nM for c-Met, 24 nM for NPM-ALK, and 11 nM for c-Met. The compound has shown significant efficacy in inhibiting tumor growth, making it a valuable tool in cancer research and therapeutic applications targeting these pathways. -
VEGFR-2/c-Met Inhibitor
Taligantinib is a selective dual inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). This orally active compound effectively suppresses tumor angiogenesis and cell proliferation. Taligantinib is of particular interest in the research of solid tumors, including non-small cell lung cancer and hepatocellular carcinoma, making it a valuable tool for cancer biology studies. -
c-Met/ALK Inhibitor
CM-118 is a selective inhibitor of c-Met and ALK, targeting the HGF-induced c-Met phosphorylation and impairing ALK phosphorylation in key variants including EML4-ALKv1, ALK F1174L, and EML4-ALKv1 L1196M. With IC50 values of 0.92, 1.25, 1.9, and 3.5 μM respectively, CM-118 demonstrates significant anticancer activity against tumors reliant on c-Met or ALK oncogenic pathways. This compound is useful for investigating therapeutic strategies in cancers driven by these targets. -
MET/VEGFR2/KDR Inhibitor
Foretinib phosphate is a potent inhibitor of the c-MET and VEGFR2 receptors, which play crucial roles in tumor growth and angiogenesis. By selectively targeting hepatocyte growth factor receptor c-MET and vascular endothelial growth factor receptor 2, Foretinib phosphate exhibits significant anti-tumor activity, potentially reducing tumor cell proliferation and metastasis. Its unique mechanism offers distinct advantages over other treatments, making it a valuable tool for research in oncology, particularly in studies related to lung cancer and the pathways involving MEK1/2, FER, and AURKB. -
ALK Inhibitor
SMU-B is a potent orally active inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of less than 0.5 nM, along with c-ros oncogene 1 (ROS1) and c-MET, exhibiting IC50 values of 1.87 nM and 28.9 nM for AXL. This compound demonstrates significant antiproliferative activity against MKN45, H1993, and H441 cell lines, with IC50s of 0.02 μM, 1.58 μM, and 2.82 μM, respectively. Additionally, SMU-B has shown promising antitumor efficacy in various mouse models, highlighting its potential for cancer research applications. -
VEGFR-2/c-Met Inhibitor
VEGFR-2/c-Met-IN-2 is a selective inhibitor targeting VEGFR-2 and c-Met, demonstrating IC50 values of 83 nM and 48 nM, respectively. This compound exhibits significant cytotoxicity against the HCT-116 cell line, with an IC50 of 3.403 µM. Its potent inhibitory effects make it a valuable tool for research into angiogenesis and cancer metastasis. -
c-Met/VEGFR-2 Inhibitor
T-1840383 is a highly potent ATP-competitive inhibitor targeting c-Met and VEGFR-2, demonstrating IC50 values of 1.9 nM for c-Met, 7.7 nM for VEGFR1, 2.2 nM for VEGFR2, and 5.5 nM for VEGFR3. This compound effectively inhibits key signaling pathways associated with cancer progression and angiogenesis. It is suitable for research applications focused on tumor growth and vascular development, making it a valuable tool in oncology and vascular biology studies. -
Stable Isotope
Crizotinib-d8 is a deuterated analog of Crizotinib, functioning as an ATP-competitive inhibitor of ALK and c-Met. This compound exhibits potent biological activity, with IC50 values of 20 nM and 8 nM, respectively, and effectively inhibits tyrosine phosphorylation of NPM-ALK and c-Met in cellular assays. Additionally, Crizotinib-d8 serves as an inhibitor of ROS1. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research involving Crizotinib to enhance understanding of its therapeutic mechanisms. -
BTK Inhibitor
Pirtobrutinib is a highly selective, non-covalent inhibitor of Bruton's tyrosine kinase (BTK). It effectively targets diverse BTK C481 substitution mutations, demonstrating strong antitumor activity in BTK-dependent lymphoma models in vivo. Pirtobrutinib exhibits over 300-fold selectivity for BTK compared to a panel of 370 other kinases and shows minimal inhibition of non-kinase off-targets at 1 μM. This specificity makes it a valuable tool for studying BTK-related signaling pathways and therapeutic applications in hematological malignancies. -
BTK Inhibitor
2-(Bromomethyl)acrylic acid functions as a selective inhibitor of Bruton's tyrosine kinase (BTK). It covalently modifies the cysteine 481 residue of BTK through a nucleophilic addition-elimination mechanism, leading to the inhibition of the B-cell receptor signaling pathway. This compound promotes immunogenic cell death in BTK-expressing B-cell lymphoma cells by triggering the release of damage-associated molecular patterns like extracellular ATP and HMGB1. It exhibits significant cytotoxicity against BTK-expressing cells while demonstrating minimal toxicity to BTK-negative counterparts, making it valuable for research into B-cell lymphoma. -
BTK Inhibitor
Acalabrutinib maleate is an oral, irreversible, and highly selective BTK inhibitor targeting cysteine residue Cys481 in the ATP-binding pocket of BTK. This compound exhibits potent activity against chronic lymphocytic leukemia (CLL) in mouse models, making it a valuable tool for CLL research. Additionally, Acalabrutinib maleate features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications. -
BTK Inhibitor
Tolebrutinib, a selective inhibitor of Bruton tyrosine kinase (BTK), demonstrates potent activity with IC50 values of 0.4 nM in Ramos B cells and 0.7 nM in HMC microglia cells. Its ability to penetrate the blood-brain barrier underscores its relevance in studying central nervous system immunity. Tolebrutinib is a valuable tool for research into multiple sclerosis (MS) and other neurological conditions influenced by BTK activity. -
BTK Degrader
Catadegbrutinib is a selective chimeric degradation activator compound targeting Bruton's tyrosine kinase (BTK), with an IC50 of 0.69 nM. By facilitating the recruitment of BTK to E3 ubiquitin ligase, Catadegbrutinib promotes polyubiquitination and subsequent proteasomal degradation of BTK, effectively reducing its activity. This compound is valuable for investigating B-cell malignancies, including chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma. -
Btk Inhibitor
BIIB091 is a selective and potent reversible Bruton’s tyrosine kinase (BTK) inhibitor, demonstrating an IC50 of less than 0.5 nM. By binding to the BTK protein and inducing an inactive conformation via sequestering of TYR-551, BIIB091 effectively obstructs BTK signaling pathways. This compound is valuable for research applications in multiple sclerosis and other immune-mediated disorders. -
PROTAC BTK Degrader
PROTAC BTK Degrader-1 is an innovative PROTAC-based compound designed for the selective degradation of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 34.51 nM for wild-type BTK and 64.56 nM for the BTK-481S mutant. This compound effectively lowers BTK protein levels, thereby inhibiting tumor growth. Additionally, PROTAC BTK Degrader-1 features an alkyne group facilitating its application in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for advanced chemical research and targeted therapies. -
BTK Inhibitor
Elsubrutinib is a potent and selective irreversible inhibitor of Bruton's tyrosine kinase (BTK). With an IC50 value of 0.18 μM for the BTK catalytic domain, it demonstrates strong inhibitory activity. Elsubrutinib is utilized in research related to inflammatory diseases, providing valuable insights into BTK's role in various cellular processes. -
HCK/BTK Inhibitor
KIN-8194 is an orally active dual inhibitor targeting HCK and BTK, exhibiting IC50 values of 0.915 nM and <0.495 nM, respectively. It effectively disrupts growth and integrin-mediated adhesion in BTK inhibitor-resistant mantle cell lymphoma (MCL). KIN-8194 demonstrates the ability to overcome ibrutinib resistance, providing a survival advantage in TMD-8 ABC DLBCL xenograft models, making it a valuable tool for research in hematologic malignancies and therapeutic resistance mechanisms. -
BTK Inhibitor
PF-06658607 is an alkynylated irreversible inhibitor of Bruton's tyrosine kinase (BTK), designed to covalently bind to active site cysteines in the ATP-binding pocket. This compound effectively serves as a research tool for identifying off-target effects of covalent kinase inhibitors in cancer cell models. Its unique alkyne functionality facilitates the use of azide-based detection probes through copper-catalyzed click chemistry, enhancing the study of BTK-related signaling pathways. -
BTK/MNK Dual Inhibitor
QL-X-138 is a selective dual inhibitor of Bruton's tyrosine kinase (BTK) and MAPK-interacting kinase (MNK), demonstrating potent covalent binding to BTK and non-covalent binding to MNK. It exhibits IC50 values of 9.4 nM for BTK, and 107.4 nM and 26 nM for MNK1 and MNK2, respectively. Additionally, QL-X-138 displays antiviral activity against dengue virus serotype 2, with an IC50 of 3.5 μM. This compound is valuable for research involving B-cell malignancies and related therapeutic investigations. -
PROTAC
L18I is a PROTAC designed to target Bruton’s tyrosine kinase (Btk), facilitating the degradation of this protein and thereby mitigating inflammation associated with autoimmune diseases, such as lupus erythematosus induced by BM12 splenocytes. This compound comprises the IBT6A ligand, a linker moiety (Propargyl-PEG3-alcohol), and an E3 ubiquitin ligase ligand (Lenalidomide-Br), effectively promoting the destruction of Btk. L18I serves as a valuable tool for investigating Btk's role in autoimmunity and offers potential pathways for therapeutic intervention. -
BTK Degrader
BTK degrader-1 is a bifunctional degrader targeting Bruton’s tyrosine kinase (BTK) through its conjugation with CD79b. This compound facilitates the targeted degradation of BTK, leading to significant anti-tumor effects. It serves as a valuable tool for research applications focused on therapeutic strategies for hematological malignancies. -
BLK Inhibitor
BLK-IN-2 is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), exhibiting an IC50 of 5.9 nM. In addition, it inhibits Bruton’s tyrosine kinase (BTK) with an IC50 of 202 nM. This compound demonstrates strong antiproliferative activity against various lymphoma cell lines, making it a valuable tool for research in B-cell malignancies and related signaling pathways. -
Covalent Probe/Btk Inhibitor
CNX-500 is a covalent probe that targets Bruton's tyrosine kinase (Btk) through a potent inhibitor (CC-292) chemically linked to biotin. With an IC50 of 0.5 nM, CNX-500 exhibits strong inhibitory activity against Btk while forming a stable covalent bond. The compound demonstrates low off-target effects on epidermal growth factor receptor and upstream Src-family kinases such as Syk and Lyn, making it suitable for research applications focused on Btk-related pathways in cellular signaling and disease models. -
BTK Inhibitor
N-piperidine Ibrutinib hydrochloride is a reversible derivative of Ibrutinib, functionally acting as a potent Bruton Tyrosine Kinase (BTK) inhibitor. It demonstrates IC50 values of 51.0 nM for wild-type BTK and 30.7 nM for the C481S mutant. This compound serves as a valuable BTK ligand in the synthesis of PROTACs, including SJF620, which has shown a DC50 of 7.9 nM, highlighting its potential utility in targeted protein degradation research applications. -
BTK Inhibitor
BIIB129 is a covalent and selectively targeting inhibitor of Bruton's tyrosine kinase (BTK), designed to penetrate the blood-brain barrier effectively. By covalently binding to Cys481 in BTK, BIIB129 disrupts the signaling pathways in B cells and myeloid cells. This compound is particularly relevant for research applications in multiple sclerosis (MS), providing insights into the modulation of immune responses associated with the disease. -
BTK Inhibitor
ACP-5862 is a potent Bruton tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 5.0 nM. As a major circulating metabolite of Acalabrutinib, it maintains high selectivity for BTK, which is critical for the modulation of B-cell signaling pathways. ACP-5862 is also a weak time-dependent inactivator of CYP3A4 and CYP2C8. This compound is widely utilized in research focused on hematological malignancies and B-cell related disorders, facilitating insights into targeted therapies. -
PROTAC BTK Degrader
DD-03-171 is a selective PROTAC BTK degrader that targets Bruton's tyrosine kinase (BTK) for degradation. This compound demonstrates significant anti-proliferative effects on mantle cell lymphoma (MCL) cells with an IC50 of 5.1 nM and enhances survival in murine models bearing patient-derived xenograft (PDX) lymphoma. Additionally, DD-03-171 inhibits platelet function and thrombosis, making it a valuable tool for research in cancer and hematological disorders. -
Stable Isotope
Acalabrutinib-d4 is a deuterated derivative of Acalabrutinib, an orally active and irreversible second-generation Bruton Tyrosine Kinase (BTK) inhibitor. This stable isotope labeled compound serves as a valuable tool for studying BTK inhibition in biological systems. Additionally, Acalabrutinib-d4 features an alkyne group, facilitating its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its applications extend to exploring therapeutic potential and pharmacokinetic properties in research settings. -
BTK Degrader
(R)-Zelebrudomide is a Bruton’s Tyrosine Kinase (BTK) degrader synthesized as an isomer of the PROTAC compound Zelebrudomide. It selectively induces the degradation of BTK, a crucial target in the treatment of various hematological malignancies. This compound is utilized in research to investigate its potential therapeutic applications in autoimmune diseases and cancers where BTK is implicated. -
Ibrutinib Derivative
Ibrutinib-MPEA is an Ibrutinib derivative targeting Bruton's tyrosine kinase (BTK), a key regulator in B cell receptor signaling. As a covalent and irreversible inhibitor, Ibrutinib-MPEA demonstrates significant biological activity against various hematological malignancies. This compound is primarily utilized in research applications focusing on cancer biology and the study of BTK-related signaling pathways. -
BTK Inhibitor
Edralbrutinib is a selective Bruton’s tyrosine kinase (BTK) inhibitor with a high potency for targeting BTK signaling pathways. This compound demonstrates significant inhibition of B-cell receptor (BCR) signaling, making it a valuable tool for studying diseases such as B-cell malignancies and autoimmune disorders. Research applications include investigation of B-cell signaling dynamics and therapeutic development for BTK-dependent pathologies. -
Btk Inhibtior
Atuzabrutinib is a selective reversible inhibitor of Bruton's tyrosine kinase (Btk), which plays a crucial role in B-cell receptor signaling. This compound demonstrates significant inhibition of neutrophil recruitment through the modulation of macrophage antigen-1 signaling pathways. Atuzabrutinib is primarily utilized in research focused on B-cell mediated autoimmunity, chronic inflammatory diseases, and various malignancies. Its targeted action on Btk makes it valuable in studying therapeutics aimed at B-cell related disorders. -
Btk Inhibitor
TAK-020 is a covalent inhibitor of Bruton's tyrosine kinase (Btk), demonstrating potent activity in targeting the Btk pathway. It is designed for use in research applications related to Btk-associated signaling in various hematological malignancies and autoimmune disorders. This compound serves as a valuable tool for investigating the role of Btk in cell proliferation and survival, making it a significant candidate for therapeutic development in these areas. -
BTK Inhibitor
JNJ-64264681 is a selective, irreversible covalent inhibitor of Bruton's Tyrosine Kinase (BTK). This compound demonstrates potent inhibition and favorable pharmacokinetic properties, making it suitable for research applications in cancer and autoimmune diseases. Its specificity for BTK allows for the exploration of pathways regulated by this critical enzyme in disease models. -
PROTAC BTK Degrader
PROTAC BTK Degrader-6 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 of 3.18 nM. This compound exhibits anti-inflammatory activity by inhibiting NF-κB activation and reducing the expression of pro-inflammatory cytokines, including IL-1β and IL-6. It serves as a valuable tool for research into the modulation of immune responses and the development of therapies for inflammatory diseases. -
BTK PROTAC Degrader
UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM, specifically designed to target Bruton's tyrosine kinase (BTK). It effectively disrupts B-cell receptor signaling and demonstrates robust degradation of both wild-type and mutant BTK proteins, including the C481S mutation. UBX-382 has been shown to inhibit tumor growth in murine xenograft models with BTK-expressing TMD-8 cells, making it a valuable tool for investigating B-cell-related malignancies and therapeutic strategies. -
Btk Inhibitor
BIIB068 is a potent and selective reversible Bruton’s Tyrosine Kinase (Btk) inhibitor, demonstrating an IC50 of 1 nM and a Kd of 0.3 nM. With over 400-fold selectivity for Btk compared to other kinases, BIIB068 is well-suited for research into autoimmune diseases. Its oral bioactivity opens avenues for studies focusing on Btk-mediated pathways and therapeutic interventions. -
BTK PROTAC Degrader
PROTAC BTK Degrader-2 is a highly effective proteolysis-targeting chimera (PROTAC) that selectively degrades Bruton's tyrosine kinase (BTK). By recruiting the Cullin-RING E3 ubiquitin ligase complex, it mediates the ubiquitination and subsequent degradation of BTK protein, leading to a marked reduction in its cellular levels. This compound is valuable in research focused on B-cell malignancies and autoimmune diseases, providing insights into BTK's role in signaling pathways and therapeutic interventions. -
Btk Inhibitor
(Rac)-Ibrutinib alkyne is a potent Bruton's tyrosine kinase (Btk) inhibitor with an IC50 of 0.72 nM. This compound effectively disrupts B-cell receptor signaling, demonstrated by an IC50 of 9 nM for inhibiting calcium flux in Ramos cells. (Rac)-Ibrutinib alkyne is suitable for investigating various Btk-related pathologies, including rheumatoid arthritis and other immune disorders. -
BTK Inhibitor
Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib, selectively targeting Bruton’s tyrosine kinase (BTK). This compound exhibits inhibitory activity towards BTK that is approximately 15 times lower than that of its parent compound, Ibrutinib. Dihydrodiol-Ibrutinib is utilized in research related to B-cell malignancies and other BTK-mediated pathways, providing insights into the modulation of immune responses and signaling pathways in cancer treatment. -
PROTAC BTK Degrader
PROTAC BTK Degrader-10 is a PROTAC agent that targets Bruton's Tyrosine Kinase (BTK) for selective degradation. This compound is particularly useful in the study of chronic lymphocytic leukemia (CLL) due to its ability to modulate BTK levels, thereby influencing malignant cell survival and proliferation. The degrader is designed with a specific ligand for BTK and a linker, enabling effective recruitment of the E3 ubiquitin ligase Cereblon for targeted degradation. -
BTK Inhibitor
BTK Inhibitor 10 is a potent and orally bioavailable inhibitor of Bruton’s tyrosine kinase (BTK), with potential applications in the treatment of rheumatoid arthritis. By selectively targeting BTK, this compound modulates B cell receptor signaling pathways, offering insights into therapeutic strategies for autoimmune diseases. Its efficacy in inhibiting BTK activity makes it a valuable tool for research in immunology and inflammation. -
GDC-0834 S-enantiomer
GDC-0834 (S-enantiomer) is a potent and selective Bruton’s tyrosine kinase (BTK) inhibitor. It demonstrates significant activity in disrupting B-cell receptor signaling, making it valuable for research focusing on B-cell malignancies and autoimmune diseases. This compound is particularly useful in studies evaluating the therapeutic potential of BTK inhibition in various hematological disorders. -
Btk Inhibitor
BTK Inhibitor 17 is a potent, orally active irreversible inhibitor of Bruton's Tyrosine Kinase (BTK), exhibiting an IC50 value of 2.1 nM. This compound demonstrates significant inhibitory activity, making it a valuable tool in the study of rheumatoid arthritis and related inflammatory diseases. Its effectiveness in BTK-related signaling pathways provides insights into therapeutic approaches for conditions associated with B-cell malignancies and autoimmune disorders. -
PROTAC Btk Degrader
SJF620 hydrochloride functions as a PROTAC designed for the degradation of Bruton's tyrosine kinase (Btk) via recruitment of the cereblon (CRBN) E3 ligase. With a DC50 value of 7.9 nM, SJF620 effectively mediates the targeted degradation of Btk, making it a valuable tool for research focused on Btk-related pathways. This compound is particularly relevant in studies of immune responses and various hematological malignancies. -
BTK Inhibitor
BGB-8035 is a highly selective bruton's tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 1.1 nM for BTK, while demonstrating lower activity against TEC and EGFR with IC50 values of 99 nM and 621 nM, respectively. This compound displays significant antitumor and anti-arthritis properties, making it a valuable tool for investigating B-cell malignancies and autoimmune diseases. BGB-8035 is ideal for research applications focused on targeted therapies in hematological tumors and related pathologies. -
Isomer
(E/Z)-Rilzabrutinib is a cis-trans isomer of the Bruton's Tyrosine Kinase (BTK) inhibitor Rilzabrutinib. This compound targets BTK, a critical regulator of B-cell receptor signaling, and plays a significant role in immune response modulation. It is utilized in research applications focused on autoimmune disorders and certain types of hematological malignancies, contributing to the understanding of BTK's role in disease pathology.
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PKC-Btk Inhibitor
Terreic acid, a quinone epoxide antibiotic, serves as a potent inhibitor of Bruton’s tyrosine kinase (Btk) by disrupting the interaction between protein kinase C (PKC) and the pleckstrin homology domain of Btk. This compound effectively inhibits the binding of GST-BtkPH to PKC in lysates of human mast cells (HMC-1), demonstrating an IC50 value of approximately 100 μM. Its ability to modulate Btk activity makes terreic acid a valuable reagent for research applications involving immune signaling and mast cell function.
