1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Btk

Btk

Bruton tyrosine kinase (Btk) is a member of the Tec family kinases with a well-characterized role in B-cell antigen receptor (BCR)-signaling and B-cell activation.

Btk plays a crucial role in B cell development and activation through the BCR signaling pathway and represents a new target for diseases characterized by inappropriate B cell activity. Btk is a kinase expressed exclusively in B cells and myeloid cells and has a well characterized, vital role in B cells highlighted by the human primary immune deficiency disease, X-linked agammaglobulinemia (XLA), which results from mutation in the Btk gene. Btk plays an essential role in the BCR signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn kinase activation, followed by Btk kinase activation. Once activated, Btk forms a signaling complex with proteins such as BLNK, Lyn, and Syk and phosphorylates phospholipase C (PLC)γ2. This leads to downstream release of intracellular Ca2+ stores and propagation of the BCR signaling pathway through extracellular signal-regulated kinase and NF-κB signaling, ultimately resulting in transcriptional changes to foster B cell survival, proliferation, and/or differentiation.

Btk Related Products (43):

Cat. No. Product Name Effect Purity
  • HY-10997
    Ibrutinib Inhibitor 99.89%
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-17600
    Acalabrutinib Inhibitor 99.94%
    Acalabrutinib is a potent, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
  • HY-19834
    Fenebrutinib Inhibitor 99.83%
    Fenebrutinib (GDC-0853) is a potent, selective, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with a Ki of 0.91 nM.
  • HY-101215
    Evobrutinib Inhibitor 98.38%
    Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC50 of 8.9 nM. Evobrutinib (M2951) has potential to treat autoimmune diseases.
  • HY-100342
    Ibrutinib-biotin Inhibitor 99.09%
    Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
  • HY-122562
    MT-802 Inhibitor
    MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
  • HY-128757
    Remibrutinib Inhibitor 98.32%
    Remibrutinib, example 6 (WO2015079417A1), is an orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.
  • HY-109010
    Poseltinib Inhibitor
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-101474A
    Zanubrutinib Inhibitor 99.45%
    Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor.
  • HY-101474
    (±)-Zanubrutinib Inhibitor 99.70%
    (±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
  • HY-15771
    Tirabrutinib Inhibitor 99.31%
    Tirabrutinib (ONO-4059) is a highly selective, orally bioavailable BTK inhibitor with an IC50 of 2.2 nM.
  • HY-112215
    ARQ 531 Inhibitor 98.54%
    ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
  • HY-109078
    Vecabrutinib Inhibitor 99.96%
    Vecabrutinib is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; Vecabrutinib shows an IC50 of 24 nM for ITK.
  • HY-18012
    Spebrutinib Inhibitor 99.69%
    Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.
  • HY-112166
    PRN1008 Inhibitor 99.49%
    PRN1008 is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • HY-112161
    Branebrutinib Inhibitor 99.56%
    Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM.
  • HY-15427
    GDC-0834 Inhibitor 99.07%
    GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
  • HY-100335
    PCI-33380 Inhibitor 98.33%
    PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
  • HY-11999
    CGI-1746 Inhibitor
    CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.
  • HY-101941
    BTK IN-1 Inhibitor 98.88%
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
Isoform Specific Products

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