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-132808
    Atuzabrutinib
    		Inhibitor 98.01%
    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-15427
    GDC-0834
    		Inhibitor 98.05%
    GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
    GDC-0834
  • HY-122830
    DD-03-171
    		Degrader 98.72%
    DD-03-171 is a BTK PROTAC degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells. (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))
    DD-03-171
  • HY-78727
    Ibrutinib deacryloylpiperidine
    		Inhibitor 99.97%
    Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib deacryloylpiperidine
  • HY-18951
    ONO-4059 analog
    		Inhibitor 99.81%
    ONO-4059 analog is an analogue of ONO-4059, and ONO-4059 (HY-15771) is a highly potent and selective Btk inhibitor.
    ONO-4059 analog
  • HY-163565
    BIIB129
    		Inhibitor 99.54%
    BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research.
    BIIB129
  • HY-101856
    BMS-986142
    		Inhibitor 99.38%
    BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
    BMS-986142
  • HY-135334
    ACP-5862
    		Inhibitor 98.41%
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862
  • 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-137438
    Edralbrutinib
    		Inhibitor 99.75%
    Edralbrutinib (TG-1701) is a potent BTK inhibitor.
    Edralbrutinib
  • HY-101793
    BMS-935177
    		Inhibitor 99.11%
    BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
    BMS-935177
  • 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-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-10997S
    Ibrutinib-d5
    		Inhibitor 98.08%
    Ibrutinib-d5 is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
    Ibrutinib-d<sub>5</sub>
  • HY-110002
    LFM-A13
    		Inhibitor 99.65%
    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 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
    LFM-A13
  • HY-101766
    Btk inhibitor 2
    		Inhibitor 99.57%
    Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2
  • HY-153220A
    (R)-NX-2127
    		Degrader 98.93%
    (R)-NX-2127 ((R)-Compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (HY-153220). (Pink: BTK ligand 10 (HY-168302); Black: (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303); Blue: Thalidomide 5-fluoride (HY-W087383).
    (R)-NX-2127
  • HY-153110
    Larotinib
    		Inhibitor 99.50%
    Larotinib 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
  • HY-163295
    BTK degrader-1
    		Degrader
    BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect.
    BTK degrader-1
  • HY-100659
    Dihydrodiol-Ibrutinib
    		Inhibitor 99.92%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity