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 (61):

Cat. No. Product Name Effect Purity
  • HY-10997
    Ibrutinib Inhibitor 99.93%
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-17600
    Acalabrutinib Inhibitor ≥98.0%
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-112215
    ARQ 531 Inhibitor 99.24%
    ARQ 531 (MK-1026) is a reversible non-covalent and orally active 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-101474A
    Zanubrutinib Inhibitor 99.18%
    Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
  • HY-19834
    Fenebrutinib Inhibitor 99.83%
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-109192
    Tolebrutinib Inhibitor 98.96%
    Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
  • HY-133137A
    SJF620 hydrochloride Inhibitor 99.28%
    SJF620 hydrochloride is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
  • HY-131342
    BIIB068 Inhibitor 99.20%
    BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
  • 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-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-109078
    Vecabrutinib Inhibitor 99.96%
    Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.
  • 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-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-129390
    Orelabrutinib Inhibitor 98.93%
    Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
  • HY-122562
    MT-802 Inhibitor 98.55%
    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-80002
    BMX-IN-1 Inhibitor 99.04%
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • 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-100335
    PCI-33380 Inhibitor 98.33%
    PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
  • HY-112646
    CG-806 Inhibitor 98.07%
    CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 µM for FLT3. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells.
  • HY-128757
    Remibrutinib Inhibitor 99.26%
    Remibrutinib, is a potent and 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.
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