Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PROTAC BTK Degrader
PTD10 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 0.5 nM and a KD of 2.28 nM. It effectively degrades BTK in Ramos and JeKo-1 cell lines, leading to the inhibition of cell growth and the induction of apoptosis through caspase activation and mitochondrial pathways. PTD10 is suitable for investigating mechanisms of B-cell dysregulation and related therapeutic strategies. -
Pirtobrutinib Enantiomer
(R)-Pirtobrutinib ((R)-LOXO-305) is an enantiomer of the BTK inhibitor Pirtobrutinib, primarily targeting Bruton's Tyrosine Kinase (BTK), which plays a critical role in B-cell receptor signaling. While exhibiting reduced activity compared to its counterpart, this compound serves as a valuable tool for studying the impact of BTK inhibition on various B-cell malignancies. It is particularly useful in research exploring resistance mechanisms associated with BTK C481 substitution mutations. -
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. -
QL47 Analogue
QL47R is an isosteric analogue of QL47, specifically designed for research involving BTK inhibition. At concentrations below 10 μM, QL47R does not exhibit significant biochemical kinase activity against BTK, nor does it demonstrate antiproliferative effects on B-Cell Lymphoma Cell Lines. This compound is useful for studies focused on the characterization of BTK-related pathways and the development of targeted therapies. -
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 PROTAC Degrader
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. -
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. -
PROTAC BTK Degrader
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. -
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. -
BTK Inhibitor
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. -
Btk Inhibitor
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. -
Btk Inhibitor
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. -
BTK Inhibitor
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. -
BTK Mutant Inhibitor
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. -
Topoisomerase I Inhibitor
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I, a key enzyme involved in DNA replication and repair. This compound disrupts the enzyme's catalytic activity, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. Topoisomerase I inhibitor 11 is primarily utilized in cancer research, particularly for studying mechanisms of drug resistance and the therapeutic potential of targeting Topoisomerase I in various malignancies. -
BTK/IKZF1/3 PROTAC Ligand
BTK/IKZF1/3 ligand 1 is a PROTAC ligand targeting Bruton's tyrosine kinase (BTK) and the Ikaros family zinc finger proteins (IKZF1/3). This compound can be conjugated with E3 ligase ligands and linkers to produce PROTAC BTK/IKZF1/3 Degrader-1, facilitating targeted protein degradation. It is valuable for cancer research, supporting investigations into therapeutic strategies aimed at modulating BTK and IKZF1/3 activity in malignant cells. -
PF-06250112 Racemate
(Rac)-PF-06250112 is a racemic mixture of PF-06250112, a highly selective and orally bioavailable inhibitor of Bruton's tyrosine kinase (BTK). This compound demonstrates potent inhibitory activity against BTK as well as BMX nonreceptor tyrosine kinase and TEC. Its selectivity and efficacy make it a valuable tool for research applications focused on B cell malignancies and other diseases associated with aberrant BTK signaling. -
BTK Inhibitor
BTK-IN-8 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), exhibiting a binding affinity with an IC50 of 0.22 nM and a Kd of 0.91 nM. This compound demonstrates significant cellular activity against whole blood CD69, with an IC50 of 0.029 µM. BTK-IN-8 is primarily used in research focused on hematological malignancies and autoimmune disorders, providing insights into BTK-mediated signaling pathways. -
BTK PROTAC Degrader
PROTAC BTK Degrader-12 is a PROTAC (Proteolysis Targeting Chimera) designed to selectively degrade Bruton's tyrosine kinase (BTK). It facilitates the targeted ubiquitination and subsequent proteasomal degradation of BTK, resulting in diminished signaling pathways associated with B-cell malignancies and autoimmune disorders. This compound serves as a valuable tool in research investigating BTK's role in disease mechanisms and therapeutic interventions. -
Btk Inhibitor
RN983 is a highly selective inhibitor of Bruton's tyrosine kinase (Btk), demonstrating potent inhibition of immunoglobulin G (IgG) production in B-cells with an IC50 of 2.5 nM, and prostaglandin D2 (PGD2) production in mast cells with an IC50 of 8.3 nM. This compound serves as a valuable tool for investigating the roles of Btk in B-cell signaling and mast cell activation, making it relevant in the study of asthma and other allergic diseases. -
BTK Inhibitor
BTK-IN-36 is a potent Bruton’s Tyrosine Kinase (BTK) inhibitor, exhibiting an IC50 of 0.5 nM. This compound effectively inhibits BTK signaling pathways, which are crucial for B-cell receptor signaling and have implications in various cancers. BTK-IN-36 is applicable in cancer research, particularly in studies exploring targeted therapies for B-cell malignancies. -
RET Inhibitor
RET-IN-14 is a highly selective RET inhibitor that demonstrates potent inhibition with IC50 values of less than 0.51 nM for wild-type RET and varying nanomolar activity against RET mutations (G810R and V804M) as well as BTK and its C481S mutant. Its exceptional efficacy positions RET-IN-14 as a valuable tool for investigating RET-driven tumors and exploring therapeutic strategies in cancer research. -
BTK Inhibitor
BTK-IN-15 is a highly potent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 value of 0.7 nM. This compound demonstrates exceptional selectivity for BTK and displays significant antitumor activity. Additionally, BTK-IN-15 is known to induce apoptosis, making it a valuable tool for research in cancer biology and the development of targeted therapies. -
BTK Inhibitor
VA5 is a potent Bruton’s tyrosine kinase (BTK) inhibitor, designed to selectively inhibit BTK activity. This compound plays a crucial role in modulating B-cell signaling pathways and has potential applications in studying various diseases associated with dysregulated BTK activity, including certain hematological malignancies and autoimmune disorders. VA5 serves as a valuable tool in preclinical research to further investigate the therapeutic potential of targeting BTK. -
BTK Degrader
PROTAC BTK Degrader-11 is a potent PROTAC designed to selectively degrade Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 1.7 nM. This compound facilitates targeted protein degradation, offering significant potential in cancer research applications by modulating BTK-related pathways. The structure includes a target protein ligand, a linker, and an E3 ligase component, allowing for effective engagement of the ubiquitin-proteasome system.
