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-17600S
    Acalabrutinib-d4
    		Inhibitor 99.50%
    Acalabrutinib-d4 (ACP-196-d4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acalabrutinib-d<sub>4</sub>
  • HY-101474B
    (R)-Zanubrutinib
    		98.97%
    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib (HY-101474A). (R)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 11 nM.
    (R)-Zanubrutinib
  • HY-136531
    XMU-MP-3
    		Inhibitor
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
    XMU-MP-3
  • HY-132879
    TAK-020
    		Inhibitor 99.93%
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
    TAK-020
  • HY-132808
    Atuzabrutinib
    		Inhibitor 98.00%
    Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling.
    Atuzabrutinib
  • HY-153245
    JNJ-64264681
    		Inhibitor 98.14%
    JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research.
    JNJ-64264681
  • 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.
    Larotinib mesylate hydrate
  • HY-149051
    BGB-8035
    		Inhibitor 99.00%
    BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.
    BGB-8035
  • HY-100659
    Dihydrodiol-Ibrutinib
    		Inhibitor 99.91%
    Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib.
    Dihydrodiol-Ibrutinib
  • HY-160966
    PROTAC BTK Degrader-10
    		Degrader 99.24%
    PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader for BTK. PROTAC BTK Degrader-10 can be used for research of chronic lymphocytic leukemia (CLL)(Pink: ligand for target protein (HY-170758); Black: linker (HY-W392857); Blue: ligand for E3 ligase Cereblon (HY-W733176))
    PROTAC BTK Degrader-10
  • HY-148066
    DB0662
    		Degrader 99.66%
    DB0662 is a multi-target kinase-directed PROTAC degrader, targeting kinases including PTK2B, MAPK9, BLK, CSK, LIMK1, etc.
    DB0662
  • HY-101522
    CHMFL-EGFR-202
    		Inhibitor 99.75%
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
    CHMFL-EGFR-202
  • HY-125997
    BTK inhibitor 10
    		Inhibitor 99.66%
    BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
    BTK inhibitor 10
  • HY-15427B
    GDC-0834 (S-enantiomer)
    GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834. GDC-0834 is a potent and selective BTK inhibitor.
    GDC-0834 (S-enantiomer)
  • HY-157763
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1
    		Degrader
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)).
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1
  • HY-131705
    BTK inhibitor 17
    		Inhibitor 99.53%
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
    BTK inhibitor 17
  • HY-131342
    BIIB068
    		Inhibitor 99.69%
    BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
    BIIB068
  • HY-133137A
    SJF620 hydrochloride
    		Inhibitor 99.28%
    SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
    SJF620 hydrochloride
  • HY-132842A
    (S)-Sunvozertinib
    		Inhibitor 99.05%
    (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
    (S)-Sunvozertinib
  • HY-151232
    (E/Z)-Rilzabrutinib
    		Inhibitor
    (E/Z)-Rilzabrutinib ((E/Z)-PRN1008) is a cis-trans isomer of Rilzabrutinib (HY-112166). Rilzabrutinib is a BTK inhibitor.
    (E/Z)-Rilzabrutinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity