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

Btk

Bruton tyrosine kinase

Btk

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-151211
    BTK-IN-16
    		Inhibitor
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia.
    BTK-IN-16
  • HY-153536
    PROTAC BTK Degrader-3
    		Inhibitor
    PROTAC BTK Degrader-3 is a potent BTK degrader with a DC50 value of 10.9 nM of BTK degradation in Mino cells. PROTAC BTK Degrader-3 has the potential for B-cell malignancies, including chronic lymphoid malignancies research.
    PROTAC BTK Degrader-3
  • HY-100659S
    Dihydrodiol-Ibrutinib-d5
    		Inhibitor
    Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib.
    Dihydrodiol-Ibrutinib-d<sub>5</sub>
  • HY-141689
    BTK-IN-3
    		Inhibitor
    BTK-IN-3 (example 1) is an inhibitor of BTK. BTK-IN-3 can used to study cancer.
    BTK-IN-3
  • HY-162280
    PROTAC BTK Degrader-9
    		Degrader
    PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model.
    PROTAC BTK Degrader-9
  • HY-168302
    BTK ligand 10
    BTK ligand 10 is the ligand of BTK. BTK ligand 10 can be used to synthesize (R)-NX-2127 (HY-153220A).
    BTK ligand 10
  • HY-168963
    PROTAC BTK Degrader-13
    		Degrader
    PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway. (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
    PROTAC BTK Degrader-13
  • HY-136113
    Ibrutinib dimer
    		Inhibitor
    Ibrutinib dimer is a Dimer of Ibrutinib. Ibrutinib dimer is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib dimer
  • HY-143716
    JAK3/BTK-IN-1
    		Inhibitor
    JAK3/BTK-IN-1 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-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002).
    JAK3/BTK-IN-1
  • HY-156743
    DCAF1 binder 2
    		Degrader
    DCAF1 binder 2, a ligands for E3 Ligase, involves in BRD9, kinase and selective BTK degration.
    DCAF1 binder 2
  • HY-151232
    Rilzabrutinib
    		Inhibitor
    Rilzabrutinib (PRN1008) is an orally active Bruton's tyrosine kinase (BTK) inhibitor with anti-inflammatory and immunomodulatory activities. Rilzabrutinib can be used in the research of various inflammatory and immune-related diseases such as acute respiratory distress syndrome and sepsis.
    Rilzabrutinib
  • HY-13036C
    (Rac)-IBT6A hydrochloride
    		Inhibitor
    (Rac)-IBT6A hydrochloride is a racemate of IBT6A hydrochloride. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    (Rac)-IBT6A hydrochloride
  • HY-160168
    BTK-IN-31
    		Inhibitor
    BTK-IN-31 (Compound 2) is a selective, non-covalently reversible, and blood-brain barrier (BBB) permeable Btk inhibitor. BTK-IN-31 has research potential in immune disorders, cancer, cardiovascular disease, viral infections, inflammation, metabolic/endocrine dysfunction, and neurological disorders.
    BTK-IN-31
  • HY-168292
    BTK ligand 9
    BTK ligand 9 is a target protein ligand for BTK and can be used to synthesize PROTAC DD-03-171 (HY-122830).
    BTK ligand 9
  • HY-10997R
    Ibrutinib (Standard)
    		Inhibitor
    Ibrutinib (Standard) is the analytical standard of Ibrutinib. This product is intended for research and analytical applications. Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib (Standard)
  • 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). Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib (Standard)
  • HY-128403
    BTK inhibitor 8
    		Inhibitor
    BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM.
    BTK inhibitor 8
  • HY-18012A
    Spebrutinib besylate
    		Inhibitor
    Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.
    Spebrutinib besylate
  • HY-18016
    CGI 560
    		Inhibitor
    CGI 560 is an inhibitor for Bruton's tyrosine kinase (BTK) with an IC50 of 400 nM.
    CGI 560
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity