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-122562
    MT-802
    		Inhibitor 98.94%
    MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
    MT-802
  • HY-18009
    (Z)-LFM-A13
    		Inhibitor 99.97%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
    (Z)-LFM-A13
  • HY-112161
    Branebrutinib
    		Inhibitor 99.82%
    Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM. Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Branebrutinib
  • HY-11999
    CGI-1746
    		Inhibitor 99.39%
    CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.
    CGI-1746
  • HY-133137
    SJF620
    		Inhibitor 98.98%
    SJF620 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
  • HY-139535
    Luxeptinib
    		Inhibitor 99.30%
    Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
    Luxeptinib
  • HY-101215
    Evobrutinib
    		Inhibitor 98.70%
    Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent BTK inhibitor, with an IC50 of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases.
    Evobrutinib
  • HY-80002
    BMX-IN-1
    		Inhibitor 99.04%
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
    BMX-IN-1
  • HY-101474
    (±)-Zanubrutinib
    		Inhibitor 99.70%
    (±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 0.63 nM.
    (±)-Zanubrutinib
  • HY-19816
    Avitinib
    		Inhibitor 99.90%
    Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects.
    Avitinib
  • HY-19816A
    Avitinib maleate
    		Inhibitor ≥98.0%
    Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.
    Avitinib maleate
  • HY-100335
    PCI-33380
    		Inhibitor ≥98.0%
    PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
    PCI-33380
  • HY-109078
    Vecabrutinib
    		Inhibitor 99.76%
    Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.
    Vecabrutinib
  • HY-10997A
    Ibrutinib Racemate
    		Inhibitor
    Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
    Ibrutinib Racemate
  • HY-43521
    Ibrutinib-MPEA
    		99.71%
    Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies.
    Ibrutinib-MPEA
  • HY-13943
    CNX-774
    		Inhibitor 99.92%
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.
    CNX-774
  • HY-139984
    BIIB091
    		Inhibitor 99.85%
    BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis.
    BIIB091
  • HY-109010
    Poseltinib
    		Inhibitor 98.08%
    Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.
    Poseltinib
  • HY-139481
    TL-895
    		Inhibitor 99.86%
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research.
    TL-895
  • HY-109143
    Elsubrutinib
    		Inhibitor ≥98.0%
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
    Elsubrutinib
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Cat. No. Product Name / Synonyms Application Reactivity