2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Btk

Btk

Bruton tyrosine kinase

Btk

Related Products

PDF 1.37 MB

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-115876
    BTK-IN-5
    		Inhibitor
    BTK-IN-5 is a covalent BTK inhibitor for researching medical conditions such as cardiovascular diseases, respiratory diseases, inflammation, and diabetes.
    BTK-IN-5
  • HY-174850
    CFON-026
    		Inhibitor
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia.
    CFON-026
  • HY-174129
    TM471-1
    		Inhibitor
    TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTKWT), >40,000 nM (BTKC481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis.
    TM471-1
  • HY-145373
    BMS-986143
    		Inhibitor
    BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
    BMS-986143
  • HY-102036
    G-744
    		Inhibitor
    G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.
    G-744
  • HY-156604
    Cinsebrutinib
    		Inhibitor
    Cinsebrutinib is a Bruton's tyrosine kinase inhibitor, extracted from patent WO2021207549 (compound 5-6). Cinsebrutinib has the potential for cancer study.
    Cinsebrutinib
  • 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-173125
    FDU73
    		Degrader
    FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity. (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))
    FDU73
  • 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-172822
    TLT8
    		Degrader
    TLT8 is a ByeTAC protein degrader targeting BTK. TLT8 non-covalently binds to Rpn-13 and BTK, thereby inducing BTK degradation. TLT8 can be used in chronic lymphocytic leukemia research. (Rpn-13 ligand: HY-159808; BTK ligand: HY-Z3101; linker: HY-172823).
    TLT8
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity