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Catalog No.
Product Name
Application
Product Information
Citations
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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 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. -
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. -
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. -
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 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. -
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 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. -
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. -
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. -
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. -
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. -
BTK Inhibitor
QL47B is a biotinylated inhibitor of Bruton's tyrosine kinase (BTK), exhibiting a potent inhibitory effect with an IC50 value of 1.3 μM. This compound demonstrates significant anti-tumor activity, making it valuable for research in cancer therapeutics and cellular signaling pathways involving BTK modulation. Its biotinylation allows for easy detection in experimental settings, enhancing its utility in biochemical assays and studies of BTK-related mechanisms. -
BTK Inhibitor
Dihydrodiol-Ibrutinib-d5 is a deuterium-labeled form of Dihydrodiol-Ibrutinib, a potent Bruton’s tyrosine kinase (BTK) inhibitor. This active metabolite exhibits inhibitory activity towards BTK that is approximately 15 times lower than that of its parent compound, ibrutinib. Dihydrodiol-Ibrutinib-d5 serves as a valuable tool for investigating the pharmacokinetics and metabolic pathways of BTK inhibition in various research applications, particularly within cancer therapeutics. -
Btk Inhibitor
(R)-Elsubrutinib is a potent Bruton tyrosine kinase (Btk) inhibitor. By selectively inhibiting Btk, this compound modulates B-cell signaling pathways, making it valuable for investigating immune disorders such as rheumatoid arthritis, psoriasis, and systemic lupus erythematosus, as well as certain malignancies. Its applications extend to preclinical research, providing insights into the therapeutic potential of targeting Btk in various disease contexts. -
BTK Inhibitor
JS25 is a selective covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 value of 5.8 nM through chelation of Tyr551. This compound demonstrates potent anti-proliferative effects on cancer cells, induces apoptosis, and has shown efficacy in promoting tumor regression in murine xenograft models of Burkitt's lymphoma. Notably, JS25 effectively crosses the blood-brain barrier, making it a valuable tool for research in brain-related malignancies. -
Btk Inhibitor
BTK inhibitor 13 is a highly potent and selective inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 value of 1.2 nM. This compound exhibits significant biological activity in modulating BTK pathways, making it a valuable tool for research in B-cell malignancies and autoimmune disorders. Its high selectivity and potency facilitate investigations into BTK's role in various signaling pathways and potential therapeutic applications. -
Btk Inhibitor
BTK-IN-5 is a covalent Bruton’s tyrosine kinase (BTK) inhibitor that effectively targets the BTK signaling pathway. This compound is instrumental in studying various medical conditions, including cardiovascular diseases, respiratory disorders, inflammation, and diabetes. Its inhibitory action on BTK makes it a valuable tool for exploring the role of BTK in disease pathogenesis and therapeutic interventions. -
BTK Inhibitor
CFON-026 is a selective, orally active non-covalent inhibitor of Bruton’s tyrosine kinase (BTK), exhibiting an IC50 of 0.27 nM. This compound demonstrates substantial antitumor efficacy against both wild-type BTK and various clinically relevant BTK resistance mutations, including C481S, T474I, L528W, and V416L. In vivo studies have shown that CFON-026 induces complete tumor regression in TMD8 xenograft models, making it a valuable tool for investigating hematological malignancies such as chronic lymphocytic leukemia and Waldenström macroglobulinemia. -
BTK Inhibitor
BMS-986143 is a potent, orally active inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.26 nM, demonstrating significant selectivity against a range of kinases. This compound also inhibits TEC, BLK, BMX, TXK, FGR, YES1, and ITK with varying IC50 values, establishing its broad-spectrum activity. BMS-986143 is valuable for research into autoimmune diseases, providing insights into the modulation of B cell signaling and function. -
BTK inhibitor
Cinsebrutinib is a selective inhibitor of Bruton's tyrosine kinase (BTK), demonstrating significant activity in disrupting BTK-mediated signaling pathways. This compound exhibits potential in cancer research, particularly in hematological malignancies, by inhibiting cell proliferation and survival. Researchers can utilize Cinsebrutinib to investigate the role of BTK in tumor biology and to explore therapeutic strategies targeting BTK in oncology. -
BTK Inhibitor
BTK-IN-14 is a potent Bruton tyrosine kinase (BTK) inhibitor, targeting the BTK signaling pathway involved in B cell antigen receptor (BCR) and Fcγ receptor (FcγR) signaling in B and myeloid cells. This compound is instrumental for the investigation of BTK's role in various pathological conditions, including autoimmune diseases, inflammatory disorders, and certain cancers. Its efficacy makes it a valuable tool for researchers exploring BTK-related therapeutic strategies. -
BTK Inhibitor
BTK-IN-20 is a selective Bruton's tyrosine kinase (BTK) inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. This compound demonstrates significant anti-inflammatory and anticancer properties, making it a valuable tool for investigating BTK's role in B-cell signaling and associated malignancies. BTK-IN-20 is suitable for research applications focusing on cancer biology and inflammation pathways. -
BTK Inhibitor
BTK-IN-27 is a potent Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 0.2 nM. It exhibits significant anti-proliferative activity in TMD8 cells, with an IC50 of less than 5 nM. This compound is suitable for research applications in cancer, lymphoma, leukemia, and immunological diseases. -
BTK Inhibitor
Midobrutinib is a potent Bruton's tyrosine kinase (BTK) inhibitor, demonstrating an IC50 of 0.813 nM. This compound is valuable for examining the role of BTK in various diseases, particularly in cancer research. By inhibiting BTK, Midobrutinib aids in the investigation of cellular signaling pathways involved in malignancies and potential therapeutic interventions. -
BTK Inhibitor
BTK-IN-11 is a selective inhibitor of Bruton's tyrosine kinase (BTK), a key enzyme in the signaling pathways of B cell antigen receptors (BCR) and Fcγ receptors (FcγR) in B cells and myeloid cells. Its potent inhibition of BTK makes it a valuable tool for investigating the role of BTK in various disease contexts, particularly autoimmune diseases, inflammatory disorders, and certain cancers. This compound supports research aimed at understanding BTK-mediated signaling and its implications in disease pathogenesis. -
GSTO1/BTK Inhibitor
GSTO1-IN-2 is a dual covalent inhibitor targeting GSTO1 and Bruton's tyrosine kinase (BTK), demonstrating IC50 values of 441 nM and 6.2 nM, respectively. This compound exhibits potent inhibitory activity, making it a valuable tool for research in oncology and autoimmunity. Its ability to effectively modulate key pathways involved in these biological processes supports investigations into therapeutic applications. -
BTK Inhibitor
BTK-IN-22 is a highly selective Bruton's tyrosine kinase (BTK) inhibitor, demonstrating an IC50 value of 0.9 nM. It also effectively inhibits BLK and BMX kinases with IC50 values of 1.4 nM and 1.2 nM, respectively. This compound is valuable for research focused on B-cell malignancies and related signaling pathways, providing a useful tool for exploring the therapeutic potential of BTK inhibition. Its improved kinase selectivity compared to existing inhibitors enhances its utility in biological studies. -
BTK Inhibitor
BTK-IN-18 is a potent, reversible Bruton’s Tyrosine Kinase (BTK) inhibitor with an IC50 of 0.002 µM. This compound effectively inhibits the expression of CD69 and CD86 in vivo, demonstrating its potential in modulating B-cell receptor signaling pathways. BTK-IN-18 is suitable for research applications in hematological malignancies and autoimmune diseases, facilitating studies on B cell function and therapy development. -
BTK Inhibitor
BTK-IN-41 is a selective Bruton’s tyrosine kinase (BTK) inhibitor with an IC50 value of 5.4 nM. This compound effectively inhibits diffuse large B cell lymphoma cell line TDM-8 with an IC50 of 13.8 nM. BTK-IN-41 is valuable for investigating the role of BTK in B cell malignancies and for evaluating potential therapeutic strategies in hematological cancers. -
Btk Inhibitor
BTK-IN-33 is a Bruton’s tyrosine kinase (Btk) inhibitor that demonstrates significant anticancer activity. This compound selectively targets the Btk pathway, which is crucial for B-cell receptor signaling and survival. BTK-IN-33 is primarily utilized in research investigating B-cell malignancies and provides potential therapeutic insights into related cancers. -
BTK Inhibitor
PF-303 is a highly selective, oral inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.64 nM. This compound forms a reversible covalent bond with the Cys481 residue of BTK, allowing for targeted modulation of BTK activity without the concerns associated with irreversible inhibitors. PF-303 is valuable for investigating the role of BTK in immune system functioning, particularly in analyzing B-cell subsets, antibody production, and T-cell activation dynamics. -
BTK Inhibitor
BTK-IN-40 is a potent Bruton’s tyrosine kinase (BTK) inhibitor, designed to selectively inhibit BTK activity. This compound exhibits significant anti-inflammatory and anti-proliferative effects, making it a valuable tool for research in autoimmune diseases and hematological malignancies. BTK-IN-40’s targeted action facilitates the exploration of BTK's role in various signaling pathways and its therapeutic potential in related conditions. -
BTK Inhibitor
WS-11 is a non-covalent reversible inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 3.9 nM and 2.2 nM for wild-type and C481S mutant BTK, respectively. Its potent activity arises from the formation of strong π-π interactions with phenylalanine 540 and p-π interactions with lysine 430 within the active site, complemented by robust hydrogen bonding. WS-11 serves as a valuable tool for studying BTK-related signaling pathways and evaluating therapeutic strategies in disorders such as lymphoma and autoimmune diseases. -
BTK Inhibitor
BTK-IN-26 is a highly potent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 0.7 nM for wild-type BTK and 0.8 nM for the C481S mutant. This compound is suitable for research in cancer and autoimmune diseases, facilitating studies on BTK's role in these conditions. Its selective inhibition allows for effective elucidation of BTK-dependent signaling pathways and therapeutic intervention. -
BTK Inhibitor
BTK-IN-34 is a selective Bruton’s Tyrosine Kinase (BTK) inhibitor. It demonstrates significant antiproliferative activity in RAMOS cells by specifically inhibiting phosphorylated BTK (Tyr223), while leaving upstream kinases Lyn and Syk unaffected. This compound is valuable for research into B cell receptor signaling and the development of therapies targeting B cell malignancies. -
BTK Inhibitor
Birelentinib is a potent, selective, non-covalent inhibitor of BTK and LYN tyrosine kinases, effective in penetrating the blood-brain barrier. It demonstrates concentration-dependent antiproliferative activity in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) lines with BTK resistance mutations, such as C481X and V416L. By disrupting both BTK-dependent and independent signaling pathways of the B-cell receptor (BCR), Birelentinib impedes tumor cell proliferation and promotes apoptosis. This compound is valuable in research aimed at overcoming resistance to existing BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL). -
BLK/BTK Inhibitor
BLK-IN-1 is a selective covalent inhibitor targeting B-Lymphoid Tyrosine Kinase (BLK) and Bruton Tyrosine Kinase (BTK), with IC50 values of 18.8 nM and 20.5 nM, respectively. This compound is valuable for investigating the role of these kinases in cancer biology and exploring potential therapeutic applications. Its specificity makes it suitable for studying the molecular mechanisms underlying malignancies associated with BLK and BTK activity. -
BTK Inhibitor
HBC-12551 is a potent orally active Bruton’s tyrosine kinase (BTK) inhibitor, demonstrating an IC50 of 1.31 nM in HEK293 cells for BTK and 2.18 nM for the BTKC481S mutant. This compound exhibits significant antitumor activity, particularly in the context of diffuse large B-cell lymphoma. HBC-12551 serves as a valuable tool for research into targeted therapies for B-cell malignancies. -
BTK Inhibitor
BTK-IN-10 is a highly potent Bruton’s Tyrosine Kinase (BTK) inhibitor, exhibiting IC50 values of less than 5 nM against both wild-type BTK and the C481S mutant variant. This compound is ideal for studying BTK signaling pathways and evaluating therapeutic strategies in hematological malignancies. Its efficacy in inhibiting BTK makes it a valuable tool for researchers investigating the role of BTK in immune regulation and cancer biology. -
Pan-BTK Inhibitor
GNE-431 is a potent, selective, noncovalent pan-BTK inhibitor that targets various BTK mutants, including C481R, T474I, and T474Ms. It demonstrates significant biological activity with an IC50 of 3.2 nM against wild-type BTK and 2.5 nM against the C481S mutant. GNE-431 is a valuable tool for research into hematological disorders and autoimmune diseases, providing insights into the modulation of B-cell signaling pathways.
