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-101521
    CHMFL-BTK-01
    		Inhibitor
    CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC50 of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation.
    CHMFL-BTK-01
  • HY-117900
    PF-06250112
    		Inhibitor
    PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively.
    PF-06250112
  • HY-147584
    BTK-IN-14
    		Inhibitor
    BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1).
    BTK-IN-14
  • HY-148832
    BTK-IN-20
    		Inhibitor
    BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation.
    BTK-IN-20
  • HY-156553
    BTK-IN-27
    		Inhibitor
    BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases.
    BTK-IN-27
  • HY-177103
    Midobrutinib
    		Inhibitor
    Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.
    Midobrutinib
  • HY-147581
    BTK-IN-11
    		Inhibitor
    BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2).
    BTK-IN-11
  • HY-143718
    JAK3/BTK-IN-3
    		Inhibitor
    JAK3/BTK-IN-3 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-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)
    JAK3/BTK-IN-3
  • HY-161876
    GSTO1-IN-2
    		Inhibitor
    GSTO1-IN-2 (Compound B-9) is a dual covalent inhibitor of GSTO1/BTK with IC50 values of 441 nM and 6.2 nM respectively.
    GSTO1-IN-2
  • HY-148585
    BTK-IN-22
    		Inhibitor
    BTK-IN-22 is a BTK inhibitor (IC50: 0.9 nM). BTK-IN-22 also inhibits BLX and BMX with IC50s of 1.4 and 1.2 nM respectively. BTK-IN-22 shows improved kinase selectivity compared to Ibrutinib (HY-10997)
    BTK-IN-22
  • HY-163183
    JAK3/BTK-IN-7
    		Inhibitor
    JAK3/BTK-IN-7 (XL-12) is a JAK3/BTK inhibitor with IC50 values of 2 nM and 14 nM, respectively. JAK3/BTK-IN-7 has anti-inflammatory activity and can be used in the study of rheumatoid arthritis.
    JAK3/BTK-IN-7
  • HY-152201
    BTK-IN-18
    		Inhibitor
    BTK-IN-18 is a potent, reversible BTK inhibitor with an IC50 of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo.
    BTK-IN-18
  • HY-171131
    BTK-IN-41
    		Inhibitor
    BTK-IN-41 (Compound 47) is the inhibitor for BTK with an IC50 of 5.4 nM. BTK-IN-41 inhibits the diffuse large B cell lymphoma cell TDM-8 with IC50 of 13.8 nM.
    BTK-IN-41
  • HY-181996
    BTK-IN-47
    		Inhibitor
    BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies.
    BTK-IN-47
  • HY-160219S
    BTK-IN-33
    		Inhibitor
    BTK-IN-33 is a Btk inhibitor with anticancer effects (WO2023174300A1; compound I).
    BTK-IN-33
  • HY-164002
    PF-303
    		Inhibitor
    PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation.
    PF-303
  • HY-170324
    BTK-IN-40
    		Inhibitor
    BTK-IN-40 (compound 375) is a BTK inhibitor.
    BTK-IN-40
  • HY-169228
    WS-11
    		Inhibitor
    WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds.
    WS-11
  • HY-153951S
    BTK-IN-26
    		Inhibitor
    BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research.
    BTK-IN-26
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity