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-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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity