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Bruton's tyrosine kinase (BTK) inhibitors act on a cytoplasmic kinase that relays signals from the B cell receptor. In 1993 two groups linked defects in the BTK gene to X-linked agammaglobulinemia, in which mature B cells fail to develop. BTK belongs to the Tec kinase family and is also expressed in myeloid cells such as macrophages and mast cells. Ibrutinib, first described as PCI-32765, binds covalently to a cysteine in the BTK active site and blocks B cell activation. Spebrutinib, listed as AVL-292 and as spebrutinib besylate, is another covalent inhibitor, while CGI1746 and RN486 bind reversibly. Ibrutinib-biotin and the fluorescent analog PCI-33380 serve as probes for BTK active-site occupancy.
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.
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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.
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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-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.
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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-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-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-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.
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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-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.
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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.
DDa-1 is a potent BTK PROTAC degrader with a DC50 of 90 nM, designed to facilitate the targeted degradation of Bruton's Tyrosine Kinase (BTK) in cellular systems. This compound effectively utilizes a novel mechanism involving DCAF1 binding, a distinct linker, and a specific BTK ligand to enhance selectivity and efficacy. DDa-1 is primarily utilized in research applications focusing on BTK-related signaling pathways and therapeutic strategies against B-cell malignancies.
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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.
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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.
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Synonyms: DZD8586
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).
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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.
BCPyr is a PROTAC-class degrader specifically targeting Bruton’s Tyrosine Kinase (BTK), exhibiting a DC50 of 800 nM. This compound integrates a BTK ligand (ligand 11) and an E3 ubiquitin ligase ligand (ligand 20) through a pyrazinyl methanol linker. BCPyr facilitates the targeted degradation of BTK, making it a valuable tool for studying diseases where BTK is implicated, such as certain hematological malignancies.
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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.
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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.
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.
BTK-IN-21 is a potent Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 33 nM. It exhibits significant inhibitory effects on BTK activity, making it a valuable tool for research applications related to cancer and autoimmune diseases. This compound enables the exploration of BTK signaling pathways and supports the development of targeted therapies in these areas.
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BTK Inhibitor 19 is a highly selective covalent inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 value of 2.7 nM. This compound effectively modulates BTK activity, playing a crucial role in pathways associated with B cell receptor signaling. It is particularly valuable in research applications focused on B cell malignancies and autoimmune diseases, facilitating the exploration of therapeutic strategies targeting BTK.
Synonyms: WS-413
Civorebrutinib is a selective inhibitor of Bruton's tyrosine kinase (Btk), which plays a critical role in B cell receptor signaling. This compound exhibits significant antineoplastic activity, making it a valuable tool for research into B cell malignancies and related disorders. Its ability to modulate B cell function positions Civorebrutinib as a candidate for studies examining targeted therapies in hematological cancers.
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RN941 is a potent Bruton's tyrosine kinase (BTK) inhibitor, targeting the BTK signaling pathway. It exhibits significant biological activity in modulating B-cell signaling, making it a valuable tool in the study of rheumatoid arthritis and B-cell malignancies. RN941 is suitable for research applications involving disease mechanisms and therapeutic strategies in these conditions.
AMX5160 is an orally active Bruton's tyrosine kinase (BTK) inhibitor, specifically targeting the mutant BTKC481S with an IC50 of 0.98 nM. This reagent is useful for investigating the role of BTK in various malignancies, including leukemia and lymphoma, as well as in research related to multiple sclerosis and other autoimmune disorders.
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