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-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 NX-2127 (HY-153220).
    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-124605
    IQS-019
    		Inhibitor
    IQS-019 is a B cell receptor (BCR) kinase inhibitor. IQS-019 can inhibit the de-phosphorylation of constitutive and IgM-activated Syk, Lyn, and Btk. IQS-019 can inhibit cell proliferation, migration and induce apoptosis. IQS-019 exhibits antitumor activity and can be used for the research of cancer, such as B cell lymphoma.
    IQS-019
  • HY-E70809
    BTK V416L Recombinant Human Active Protein Kinase
    Bruton's tyrosine kinase (BTK) plays a vital role in B-cell antigen receptor (BCR) signalling transduction pathway. BTK can be used for the study of lymphomas and autoimmune diseases. BTK has multiple mutants. BTK V416L Recombinant Human Active Protein Kinase is a recombinant BTK V416L protein that can be used to study BTK V416L-related functions.
    BTK V416L Recombinant Human Active Protein Kinase
  • 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-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-176526
    BTK degrader-1 intermediate
    		Degrader
    BTK degrader-1 intermediate (compound 5) is an intermediate for the synthesis of BTK degrader-1 (HY-163295). BTK degrader-1 can be used as an ADC toxin to synthesize antibody-drug conjugate (ADC).
    BTK degrader-1 intermediate
  • 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-135334S
    ACP-5862-d4
    		Inhibitor
    ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862-d<sub>4</sub>
  • 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
  • HY-10997AR
    Ibrutinib Racemate (Standard)
    		Inhibitor
    Ibrutinib (Racemate) (Standard) is the analytical standard of Ibrutinib (Racemate). This product is intended for research and analytical applications. Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
    Ibrutinib Racemate (Standard)
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Cat. No. Product Name / Synonyms Application Reactivity