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-101474S
    Zanubrutinib-d5
    		Inhibitor 99.0%
    Zanubrutinib-d5 is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor.
    Zanubrutinib-d<sub>5</sub>
  • HY-110013
    Terreic acid
    		Inhibitor
    Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM.
    Terreic acid
  • HY-160246
    QL47B
    		Inhibitor
    QL47B, a biotinylated analogue of QL47 (HY-80003), is a potent inhibitor of BTK, with an IC50 value of 1.3 μM. QL47B has anti-tumor activity.
    QL47B
  • HY-154860
    PTD10
    		Degrader
    PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease.
    PTD10
  • HY-131328A
    (R)-Pirtobrutinib
    		99.78%
    (R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations.
    (R)-Pirtobrutinib
  • HY-10997S
    Ibrutinib-d5
    		Inhibitor 98.08%
    Ibrutinib-d5 (PCI-32765-d5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
    Ibrutinib-d<sub>5</sub>
  • HY-15427A
    GDC-0834 Racemate
    		98.04%
    GDC-0834 Racemate is the racemic form of GDC-0834 (HY-15427). GDC-0834 is an orally active selective, potent, and reversible BTK inhibitor with an IC50 of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA).
    GDC-0834 Racemate
  • HY-100659S
    Dihydrodiol-Ibrutinib-d5
    		Inhibitor 99.19%
    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-109143B
    (R)-Elsubrutinib
    		Inhibitor 98.0%
    (R)-Elsubrutinib ((R)-ABBV-105) is a Btk inhibitor. (R)-Elsubrutinib can be used in studies of immune diseases (such as rheumatoid arthritis, psoriasis, ankylosing spondylitis, asthma, systemic lupus erythematosus) and cancer.
    (R)-Elsubrutinib
  • HY-136113
    Ibrutinib dimer
    		Inhibitor 98.27%
    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-13036
    (Rac)-IBT6A
    		Inhibitor 98.18%
    (Rac)-IBT6A is a racemate of IBT6A. 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
  • HY-160246A
    QL47B TFA
    		Inhibitor
    QL47B TFA, a biotinylated analogue of QL47 (HY-80003), is a potent inhibitor of BTK, with an IC50 value of 1.3 μM. QL47B TFA has anti-tumor activity.
    QL47B TFA
  • 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-13036B
    IBT6A hydrochloride
    		Inhibitor 99.35%
    IBT6A hydrochloride 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.
    IBT6A hydrochloride
  • HY-160245
    QL47R
    		99.94%
    QL47R is an approximately isosteric analogue of QL47 (HY-80003). QL47R dose not inhibit the biochemical kinase activity of BTK at concentrations below 10 μM. QL47R dose not display antiproliferative activity on B-Cell Lymphoma Cell Lines at concentrations of less than 10 μM.
    QL47R
  • HY-156746
    DBt-10
    		Degrader
    DBt-10 is a potent BTK PROTAC degrader (DC50: 137 nM). Blue: DCAF1 binder (HY-149934); Black: linker; Pink: BTK ligand.
    DBt-10
  • HY-151808
    JS25
    		Inhibitor 98.37%
    JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551. JS25 inhibits cancer cells proliferation, pronounces cell death, and promotes murine xenograft model of Burkitt’s lymphoma. JS25 effectively crosses the blood-brain barrier.
    JS25
  • HY-132196
    BTK inhibitor 18
    		Inhibitor
    BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
    BTK inhibitor 18
  • HY-130255
    BTK inhibitor 13
    		Inhibitor
    BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM.
    BTK inhibitor 13
  • HY-111781
    Civorebrutinib
    		Inhibitor
    Civorebrutinib (WS-413) is a selective, orally active BTK and TEC inhibitor with an IC50 of <100 nM for both targets. Civorebrutinib inhibits B cell activation. Civorebrutinib significantly suppresses the in vivo growth of diffuse large B-cell lymphoma cells. Civorebrutinib can be used for the research of diffuse large B-cell lymphoma.
    Civorebrutinib
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