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-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
  • 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-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-156745
    DDa-1
    		Degrader
    DDa-1 is a potent BTK degrader (DC50: 90 nM). Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BTK ligand (HY-107447).
    DDa-1
  • HY-171893
    CRBN ligand-185
    		Ligand
    CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948 (HY-153321).
    CRBN ligand-185
  • HY-155072
    PROTAC BTK Degrader-5
    		Degrader
    PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898))1.
    PROTAC BTK Degrader-5
  • 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-162407
    I-As-1
    		Inhibitor
    I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively.
    I-As-1
  • HY-162257
    BTK-IN-34
    		Inhibitor
    BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway.
    BTK-IN-34
  • HY-160167
    Birelentinib
    		Inhibitor
    Birelentinib (compound cpd15) is an inhibitor of Bruton's tyrosine kinase (BTK) and mutant BTK with IC50 values of 6.72 and 6.11 nM, respectively.
    Birelentinib
  • HY-151920
    BTK-IN-17
    		Inhibitor
    BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects.
    BTK-IN-17
  • HY-144283
    BLK-IN-1
    		Inhibitor
    BLK-IN-1 (compound 1) is a selective and covalent inhibitor of B-Lymphoid tyrosine kinase (BLK) and BTK, with IC50s of 18.8 nM and 20.5 nM, respectively. BLK-IN-1 can be used for the research of cancer.
    BLK-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity