Tag: BTK

Tirabrutinib is a Selective BTK Inhibitor

The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...

Pirtobrutinib is an Orally Active, Highly Selective and non-Covalent BTK Inhibitor

Bruton’s tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic signaling. It is critical for the proliferation and survival of leukemic cells in many B cell malignancies. BTK has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases...

SJF620 is a Potent PROTAC BTK Degrader

Bruton’s tyrosine kinase (BTK) is an enzyme encoded by the BTK gene in human. BTK is critical for the survival of B-cell neoplasms. BTK plays a crucial role in B cell development, differentiation, and signaling. Inhibition of BTK kinase activity is an important and practical way of treating Non-Hodgkin’s...

XMU-MP-3 is a Potent Non-Covalent BTK Inhibitor and Induces Apoptosis

BTK, a nonreceptor tyrosine kinase member of the Tec kinase family, plays a significant role in B-cell development. BTK is a unique therapeutic target in B-cell malignancies. XMU-MP-3, a noncovalent inhibitor with potent BTK inhibitory. XMU-MP-3 suppresses BTK kinase activity both in vitro and in vivo. In addition, XMU-MP-3...

CNX-500 is a Covalent Btk Inhibitor (CC-292) Linked to Biotin Chemically

Bruton’s tyrosine kinase (Btk) is a kinase. B cells and myeloid cells expressed exclusively. It plays a vital role in B cells. Btk plays an essential role in the B cell receptor (BCR) signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn...

MT-802 is a PROTAC Degrader of BTK for C481S Mutant CLL Treatment

The irreversible inhibitor Ibrutinib for Bruton’s tyrosine kinase (BTK) has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies. However, more than 80% of CLL patients develop resistance due to the mutant site in cysteine to serine covalently bound by Ibrutinib...