1. Protein Tyrosine Kinase/RTK
  2. 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 (170):

Cat. No. Product Name Effect Purity
  • HY-101474A
    Zanubrutinib Inhibitor 99.18%
    Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC50: 0.3 nM)[1][2].
  • HY-19834
    Fenebrutinib Inhibitor 99.42%
    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[1].
  • HY-17600
    Acalabrutinib Inhibitor
    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)[1][2]. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-131328
    Pirtobrutinib Inhibitor 99.88%
    Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM[1].
  • HY-10997
    Ibrutinib Inhibitor 99.93%
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM[1].
  • HY-164002
    PF-303 Inhibitor
    PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation[1][2].
  • HY-17600R
    Acalabrutinib (Standard) Inhibitor
    Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. 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)[1][2]. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-163565
    BIIB129 Inhibitor
    BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research[1].
  • HY-147584
    BTK-IN-14 Inhibitor
    BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1)[1].
  • HY-122830
    DD-03-171 Degrader
    DD-03-171 is a BTK, IKFZ1 and IKFZ3 degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells[1].
  • HY-149391
    PROTAC BTK Degrader-6 Degrader
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6)[1].
  • HY-148832
    BTK-IN-20 Inhibitor
    BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation[1].
  • HY-156553
    BTK-IN-27 Inhibitor
    BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases[1].
  • HY-147581
    BTK-IN-11 Inhibitor
    BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2)[1].
  • HY-139481
    TL-895 Inhibitor 99.86%
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively[1]. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research[2][3][4].
  • HY-122828
    PROTAC BTK Degrader-2 Degrader
    PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels[1].
  • HY-156746
    DBt-10 Degrader
    DBt-10 is a potent BTK degrader[1].
  • HY-143718
    JAK3/BTK-IN-3 Inhibitor
    JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)[1]
  • HY-153110A
    Larotinib mesylate hydrate Inhibitor 98.66%
    Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1].
  • HY-18009
    (Z)-LFM-A13 Inhibitor 99.97%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.