1. Protein Tyrosine Kinase/RTK
  2. Btk


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.

Btk 相关产品 (35):

Cat. No. Product Name Effect Purity
  • HY-10997
    PCI-32765 Inhibitor 99.89%
    PCI-32765 是具有选择性的 Btk 的不可逆抑制剂,IC50 值为 0.5 nM。
  • HY-17600
    Acalabrutinib Inhibitor 99.67%
    Acalabrutinib 是一种新颖的,有效的,选择性的 BTK 抑制剂,在人全血 CD69 B 细胞激活试验中,IC50EC50 分别为 3 nM 和 8 nM。
  • HY-19834
    GDC-0853 Inhibitor 99.50%
  • HY-18012
    AVL-292 Inhibitor 99.95%
    AVL-292 是一种有效的 Btk 激酶活性抑制剂,IC50<0.5 nM,Kinact/Ki 为 7.69×104 M-1s-1s。
  • HY-101215
    Evobrutinib Inhibitor 98.17%
    Evobrutinib是BTK的抑制剂, 来自专利US20140162983 化合物实例0174。
  • HY-109078
    Vecabrutinib Inhibitor 99.13%
    Vecabrutinib 是一种有效的,非共价的 BTKITK 抑制剂,Kd 值分别为 0.3 nM 和 2.2 nM;Vecabrutinib 对 ITK 的 IC50 值为 24 nM。
  • HY-112646
    CG-806 Inhibitor
    CG-806 是 FLT3/BTK 等多种激酶的抑制剂。
  • HY-101856
    BMS-986142 Inhibitor
    BMS-986142 是一种有效的、具有高选择性的 Bruton's 酪氨酸激酶 (BTK) 可逆性抑制剂,其 IC50值为 0.5 nM。
  • HY-15771
    ONO-4059 Inhibitor 98.31%
    ONO-4059是一个高的,有选择性的BTK抑制剂,IC50值是2.2 nM.
  • HY-100342
    Ibrutinib-biotin Inhibitor 99.67%
    Ibrutinib-biotin 是一种由 Ibrutinib 通过长链接头连接到生物素上组成的探针,具体可参考 WO2014059368A1 中 Compound 1-5,抑制 BTKIC50 值为 0.755-1.02 nM。
  • HY-80002
    BMX-IN-1 Inhibitor 98.88%
    BMX-IN-1 是一种选择性的,不可逆的 bone marrow tyrosine kinase on chromosome X (BMX) 抑制剂,在BMX ATP结合域中,靶作用于 Cys496IC50 值为 8 nM;同时作用于 BTKIC50 值为 10.4 nM。
  • HY-101474
    (±)-Zanubrutinib Inhibitor 99.70%
    (±)-Zanubrutinib 是一种有效的选择性 Bruton's 酪氨酸激酶 (Btk) 抑制剂。
  • HY-15427
    GDC-0834 Inhibitor 99.07%
    GDC-0834 是一种有效的选择性 BTK 抑制剂。GDC-0834 抑制 BTK,在体外酶实验和细胞实验中,IC50 分别为 5.9 和 6.4 nM,而在小鼠和大鼠体内,IC50 分别为 1.1 和 5.6 μM。
  • HY-18018
    RN486 Inhibitor 99.38%
    RN486是高活性Btk抑制剂,IC50为4.0 nM。
  • HY-101941
    BTK IN-1 Inhibitor 98.88%
    BTK IN-1 是一种有效的 BTK 抑制剂,IC50 值 <100 nM。
  • HY-18009
    LFM-A13 Inhibitor 99.70%
    LFM-A13 是一种有效的 BTKJAK2PLK 抑制剂,可抑制 BTK,Plx1 和 PLK3 的活性,IC50 分别为 2.5 μM,10 μM 和 61 μM。
  • HY-10997A
    PCI-32765 Racemate Inhibitor
    PCI-32765 (Ibrutinib) Racemate是PCI-32765的外消旋体。PCI-32765是Btk选择性抑制剂,IC50为0.5 nM,对Bmx,CSK,FGR,BRK,HCK有中度抑制性,但对EGFR,Yes, ErbB2,JAK3抑制性则较弱。
  • HY-11999
    CGI-1746 Inhibitor
    CGI-1746 是一种有效的,高选择性的 Btk 抑制剂,IC50 值为 1.9 nM。
  • HY-15771A
    ONO-4059 hydrochloride Inhibitor 98.74%
    ONO-4059的IC50值是2.2 nm,是一种有选择性和新颖的抑制剂。 在B细胞中ONO-4058结合BTK,因此阻止B细胞受体信号和阻碍B细胞的发展。
  • HY-80003
    QL47 Inhibitor 99.03%
    QL47不可逆的BTK抑制剂,IC50为7 nM。
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