BTK

Cat. No.

A34397

CAS No.

2770960-52-4

BIIB129

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.

Cat. No.

A34398

CAS No.

2230757-47-6

ACP-5862

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.

Cat. No.

A34402

CAS No.

1710768-30-1

Ibrutinib-MPEA

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.

Cat. No.

A34403

CAS No.

1858206-58-2

Edralbrutinib

Synonyms: TG-1701

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.

Cat. No.

A34404

CAS No.

1581714-49-9

Atuzabrutinib

Synonyms: SAR 444727; PRN473

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.

Cat. No.

A34406

CAS No.

1627603-21-7

TAK-020

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.

Cat. No.

A34407

CAS No.

2101524-34-7

JNJ-64264681

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.

Cat. No.

A34410

CAS No.

1798787-27-5

BIIB068

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.

Cat. No.

A34412

CAS No.

936563-91-6

(Rac)-Ibrutinib alkyne

(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.

Cat. No.

A34413

CAS No.

1654820-87-7

Dihydrodiol-Ibrutinib

Synonyms: PCI-45227

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.

Cat. No.

A34415

CAS No.

2241732-30-7

BTK inhibitor 10

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.

Cat. No.

A34416

CAS No.

1133432-50-4

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.

Cat. No.

A34417

CAS No.

1858206-76-4

BTK inhibitor 17

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.

Cat. No.

A34419

CAS No.

2283349-24-4

BGB-8035

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.

Cat. No.

A34420

CAS No.

1575591-66-0

(E/Z)-Rilzabrutinib

Synonyms: (E/Z)-PRN1008

(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.

Cat. No.

A34421

CAS No.

121-40-4

Terreic acid

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.

Cat. No.

A34422

CAS No.

1579278-92-4

QL47B

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.

Cat. No.

A34424

CAS No.

2101700-14-3

(R)-Pirtobrutinib

Synonyms: (R)-LOXO-305

(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.

Cat. No.

A34427

CAS No.

1643570-23-3

(R)-Elsubrutinib

Synonyms: (R)-ABBV-105

(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.

Cat. No.

A34429

CAS No.

2411771-95-2

JS25

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.

Cat. No.

A34430

CAS No.

2376726-26-8

BTK inhibitor 13

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.

Cat. No.

A34431

CAS No.

2145152-06-1

BTK-IN-5

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.

Cat. No.

A34432

CAS No.

2941611-57-8

CFON-026

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.

Cat. No.

A34433

CAS No.

1643372-83-1

BMS-986143

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.

Cat. No.

A34434

CAS No.

2724962-58-5

Cinsebrutinib

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.