BTK

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 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.

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.

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.

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-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.

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-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-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-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.

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-IN-38 is a potent inhibitor of Bruton's tyrosine kinase (BTK). It effectively inhibits the proliferation of DOHH2 and BT474 cancer cell lines, exhibiting IC50 values of 114 nM and 340 nM, respectively. This compound is of particular interest in research applications targeting B-cell malignancies and related signaling pathways.

BTK-IN-23 is a selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 12.8 nM. This compound also exhibits inhibitory effects on BMX and BLK, with IC50 values of 5.7 nM and 35.6 nM, respectively. BTK-IN-23 demonstrates enhanced kinase selectivity compared to Ibrutinib, making it a valuable tool for research in cancer and autoimmune disease therapies, particularly in studies focusing on B-cell signaling pathways.

BTK-IN-43 is a selective inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 value of 21.6 nM. This compound is capable of oral administration and exhibits potent activity against BTK-mediated signaling pathways. It is primarily utilized in research applications focused on hematological malignancies and immune disorders driven by aberrant BTK activity.

HZ-A-005 is a potent and selective covalent inhibitor of Bruton’s tyrosine kinase (BTK), a critical regulator in B cell receptor signaling. This compound demonstrates significant anti-tumor activity, effectively reducing tumor growth in xenograft mouse models. HZ-A-005 is valuable for research applications focused on B cell malignancies and the study of BTK's role in various signaling pathways.

BTK-IN-32 is a selective Bruton’s tyrosine kinase (BTK) inhibitor that effectively modulates BTK activity. It uniquely activates both full-length BTK and smaller multidomain fragments, rather than solely targeting the isolated kinase domain. This compound is useful in research applications focused on B-cell signaling pathways and the development of therapies for related hematological malignancies.

BTK Inhibitor 20 is a highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), exhibiting an IC50 value of 8 nM. This compound effectively modulates the BTK signaling pathway, playing a critical role in B-cell receptor signaling and related processes. It is valuable for research focused on B-cell malignancies, autoimmune diseases, and other conditions where BTK activity is implicated.

BTK-IN-25 is a highly potent inhibitor of Bruton’s tyrosine kinase (BTK), demonstrating an IC50 of 0.77 nM against the BTK(C481S) mutant and 1 nM in DOHH2 cells. This compound is valuable for exploring BTK-related signaling pathways and potential therapeutic interventions in B-cell malignancies. Its selective inhibition of BTK makes it a useful tool for research applications focused on the modulation of immune responses and the development of targeted cancer therapies.

BTK-IN-12 is a potent Bruton’s Tyrosine Kinase (BTK) inhibitor, with IC50 values of 1.2 nM for wild-type BTK and 0.8 nM for the mutated BTK (C481S). This compound selectively targets BTK, a key regulator in B-cell receptor signaling, making it valuable for research in hematological malignancies and autoimmune disorders. BTK-IN-12 can facilitate the study of therapeutic approaches for conditions associated with dysregulated B-cell activity.

ABBV-992 is a potent and selective Bruton's Tyrosine Kinase (BTK) inhibitor. It demonstrates significant inhibitory activity, making it a valuable tool for studying various hematological malignancies. This compound is primarily utilized in cancer research to investigate BTK signaling pathways and their roles in tumor progression and survival.

(R)-Acalabrutinib is a specific inhibitor of Bruton’s tyrosine kinase (BTK), a critical protein involved in B-cell receptor signaling. This compound serves as a valuable tool for research applications in hematological malignancies, particularly in the study of B-cell functions and the development of targeted therapies for conditions such as non-Hodgkin lymphoma and chronic lymphocytic leukemia. Its high selectivity for BTK allows for detailed investigations into BTK-mediated pathways and potential therapeutic interventions.

BTK-IN-19 is a reversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of less than 0.001 μM. This compound demonstrates potent inhibitory activity against BTK, making it a valuable tool for studying B-cell signaling pathways. BTK-IN-19 is applicable in research focused on various hematological malignancies and autoimmune diseases, contributing to the understanding of therapeutic strategies targeting BTK.

BTK-IN-16 is a dual inhibitor targeting Bruton’s tyrosine kinase (BTK), specifically effective against both wild type and the C481S mutant, with IC50 values of 5.1 μM and 4.1 μM, respectively. This compound is crucial for research into autoimmune diseases and chronic lymphocytic leukemia, where BTK plays a significant role in disease progression. Its ability to inhibit both forms of BTK makes BTK-IN-16 a valuable tool for studying therapeutic strategies in these conditions.

BTK-IN-3 is a selective inhibitor of Bruton's tyrosine kinase (BTK), a critical component in B-cell receptor signaling. This compound demonstrates significant biological activity by inhibiting BTK-mediated pathways, which are often implicated in various hematological malignancies. BTK-IN-3 is therefore utilized in research applications focused on cancer biology, particularly in the investigation of B-cell cancers and autoimmune disorders.

Ibrutinib dimer is a dimeric form of Ibrutinib, a selective and irreversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 0.5 nM. This compound serves as a valuable tool for studying Btk-mediated signaling pathways and its implications in various hematological malignancies. Researchers can utilize Ibrutinib dimer to investigate the effects of Btk inhibition in cellular models and to explore its potential therapeutic applications in cancer research.

(Rac)-IBT6A hydrochloride is a racemic mixture of IBT6A, a byproduct of Ibrutinib. This compound acts as a selective, irreversible Bruton's tyrosine kinase (Btk) inhibitor with an IC50 of 0.5 nM, making it useful for studying Btk-mediated signaling pathways. It serves as a valuable reagent in the synthesis of Ibrutinib derivatives and adducts, facilitating research into therapeutic strategies for diseases such as B-cell malignancies.

(R,R)-Birelentinib is a potent Bruton's tyrosine kinase (BTK) inhibitor, achieving IC50 values of 0.7 nM for wild-type BTK and 0.86 nM for the C481S mutant. This compound effectively inhibits the self-phosphorylation of BTK, with an IC50 of 24.3 nM. (R,R)-Birelentinib demonstrates significant anti-proliferative effects against wild-type and C481S mutant HEK293 cells, making it valuable for research into drug-resistant B-cell malignancies.

CGI 560 is a potent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 value of 400 nM. This compound plays a significant role in the modulation of B-cell receptor signaling pathways, making it a valuable tool for research in hematological malignancies and autoimmune diseases. Its ability to selectively inhibit BTK can aid in elucidating the mechanistic underpinnings of various B-cell-related disorders.

Btk inhibitor 1 R enantiomer (Ibrutinib analog) (Compound 14) is a covalent and irreversible Bruton??s tyrosine kinase (BTK) inhibitor and can be used in synthesis of Ibrutinib and ibrutinib-based activity-based probes (ABPs).

Btk inhibitor 1 R enantiomer hydrochloride (Ibrutinib analog hydrochloride) (Compound 14) is a covalent and irreversible Bruton??s tyrosine kinase (BTK) inhibitor and can be used in synthesis of Ibrutinib and ibrutinib-based activity-based probes (ABPs).

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor.

Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity.

Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM.

Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.

BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.

TM471-1 is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK), demonstrating an IC50 of 1.3 nM against BTKWT and exhibiting selectivity with IC50 values of >40,000 nM for BTKC481S, 7.9 nM for TEC, and 12.4 nM for TXK. This compound effectively inhibits cell proliferation both in vivo and in vitro, induces apoptosis, and causes arrest in the G0/G1 phase of the cell cycle. TM471-1 is valuable for research into the roles of BTK in various cancer types and related signaling pathways.

Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy.

Sunvozertinib (DZD9008) is a potent, orally active inhibitor of ErbB family kinases, including mutant forms of EGFR and HER2, as well as Bruton's tyrosine kinase (BTK). It demonstrates strong inhibitory activity against a range of clinically relevant EGFR mutations, with IC₅₀ values of 20.4 nM for EGFR exon 20 NPH insertion, 20.4 nM for EGFR exon 20 ASV insertion, 1.1 nM for EGFR L858R/T790M, and 7.5 nM for HER2 exon 20 YVMA mutation. It exhibits reduced activity against wild-type EGFR (IC₅₀ = 80.4 nM in A431 cells), supporting its selectivity for mutant forms. Sunvozertinib is being investigated as a targeted therapy for non-small cell lung cancers harboring EGFR or HER2 exon 20 alterations.

Zelebrudomide (NX-2127) is a novel, potent BTK degrader that induces proteasomal degradation through targeted ubiquitination, rather than direct inhibition. In addition to degrading BTK, Zelebrudomide (NX-2127) enhances immune responses by stimulating T cell activation and increasing IL-2 production in primary human T cells, supporting its potential in cancer and immunotherapy research.

PLS-123 is a covalent, irreversible inhibitor of Bruton's tyrosine kinase (BTK), displaying an IC50 of less than 5 nM. It effectively disrupts BTK's catalytic activity at Tyr551 and self-activation at Tyr223, leading to the inhibition of key signaling pathways, including AKT/mTOR and MAPK, as well as blocking PLCγ2 activation. PLS-123 exhibits potent anti-proliferative effects against a range of B-cell lymphoma cell lines, inducing apoptosis through a caspase-dependent mechanism. Additionally, it demonstrates substantial antitumor efficacy in the OCI-Ly7 xenograft model, making it a valuable tool for research in lymphoma.

TL-895 is a potent, orally bioavailable, irreversible inhibitor of Bruton's tyrosine kinase (BTK) that functions as an ATP-competitive agent. It demonstrates high selectivity with an average IC50 of 1.5 nM against recombinant BTK and minimal activity against BLK, BMX, and TXK. TL-895 effectively inhibits BTK auto-phosphorylation at the Y223 site (IC50: 1-10 nM) and suppresses the production of inflammatory cytokines such as IL-8, IL-1β, MCP-1, and TNF-α in monocytes and macrophages. This compound is valuable for investigating chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and various B-cell malignancies.

XMU-MP-3 is a potent non-covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 10.7 nM for wild-type BTK and 17.0 nM for the C481S mutation in the presence of 10 μM ATP. This compound is known to induce apoptosis in BTK-dependent cells, making it a valuable tool for investigating B-cell receptor signaling and related pathways. XMU-MP-3 is applicable in research focused on hematological malignancies and immune responses.

EGFR-IN-40 is a selective inhibitor targeting Bruton's tyrosine kinase (BTK), epidermal growth factor receptor (EGFR), and IL-2-inducible T-cell kinase (ITK). It exhibits potent inhibitory activity with IC50 values of 1.2 nM for BTK, 5.3 nM for EGFR, and 46.1 nM for ITK. This compound is valuable for research applications focusing on cancer therapeutics and signaling pathways related to these kinases.

(S)-Sunvozertinib, the S-enantiomer of Sunvozertinib, acts as a selective inhibitor of the ErbB family of receptors and Bruton's tyrosine kinase (BTK). It demonstrates potent inhibitory activity against multiple oncogenic variants of EGFR, including exon 20 insertions and the L858R/T790M mutation, with IC50 values of 51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively. Due to its dual action on both ErbBs and BTK, (S)-Sunvozertinib is poised for applications in targeted cancer therapy and research into mechanisms of resistance in EGFR-driven malignancies.

Rocbrutinib is a highly selective Bruton's tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 0.11 nM for wild-type BTK and 1.0 nM for the C481S-mutated variant. It demonstrates significant anti-leukemic activity by reducing cell viability, inducing cytotoxic effects, and inhibiting cell migration. This compound is applicable in research surrounding chronic lymphocytic leukemia, non-Hodgkin's lymphoma, and mantle cell lymphoma.

BTK-IN-48 is a potent inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 1.14 μM. This compound effectively inhibits recombinant BTK and c-Src, demonstrating moderate activity against LCK, BMX/ETK, FLT3, and PIM1. BTK-IN-48 is valuable for research related to B-cell malignancies and autoimmune diseases, making it a useful tool for understanding the underlying mechanisms of these conditions.