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-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-124645
    QL-X-138
    		Inhibitor 98.17%
    QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.
    QL-X-138
  • HY-18018
    RN486
    		Inhibitor 98.91%
    RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.
    RN486
  • HY-101474AR
    Zanubrutinib (Standard)
    		Inhibitor
    Zanubrutinib (Standard) is the analytical standard of Zanubrutinib. This product is intended for research and analytical applications. Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC50: 0.3 nM).
    Zanubrutinib (Standard)
  • HY-135334
    ACP-5862
    		Inhibitor 98.32%
    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-43521
    Ibrutinib-MPEA
    		Inhibitor 99.71%
    Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases.
    Ibrutinib-MPEA
  • HY-18010
    PCI 29732
    		Inhibitor 99.59%
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
    PCI 29732
  • HY-130983
    N-piperidine Ibrutinib hydrochloride
    		Inhibitor 98.06%
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
    N-piperidine Ibrutinib hydrochloride
  • HY-15809
    (Rac)-Ibrutinib alkyne
    		Inhibitor 99.35%
    (Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC50 of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis.
    (Rac)-Ibrutinib alkyne
  • HY-137438
    Edralbrutinib
    		Inhibitor 99.75%
    Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma.
    Edralbrutinib
  • HY-153220A
    (R)-Zelebrudomide
    		Degrader 98.93%
    (R)-Zelebrudomide ((R)-NX-2127) ((R)-Compound 28) is an isomer of the BTK PROTAC degrader Zelebrudomide (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)-Zelebrudomide
  • HY-150023
    BI-1622
    		Inhibitor 98.02%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-101793
    BMS-935177
    		Inhibitor 98.35%
    BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
    BMS-935177
  • 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-149391
    PROTAC BTK Degrader-6
    		Degrader 99.24%
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6).
    PROTAC BTK Degrader-6
  • HY-122828
    PROTAC BTK Degrader-2
    		Degrader 99.93%
    PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels.
    PROTAC BTK Degrader-2
  • HY-101941
    BTK IN-1
    		Inhibitor 98.09%
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
    BTK IN-1
  • HY-160142
    UBX-382
    		Degrader
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers.
    UBX-382
  • 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 99.53%
    Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity