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  1. Protein Tyrosine Kinase/RTK
  2. Btk

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 (37):

Cat. No.Product NameEffectPurity
  • HY-10997
    IbrutinibInhibitor 99.89%
    Ibrutinib (PCI-32765) 是选择性,不可逆的 Btk抑制剂,IC50 值为 0.5 nM。
  • HY-17600
    AcalabrutinibInhibitor 99.94%
    Acalabrutinib 是一种新颖的,有效的,选择性的 BTK抑制剂,在体内试验中IC50EC50 分别为 3 nM 和 8 nM。
  • HY-19834
    FenebrutinibInhibitor 99.50%
    Fenebrutinib (GDC-0853) 是有效,选择性和非共价的布鲁顿酪氨酸激酶 (Btk) 抑制剂,Ki 为0.91 nM。
  • HY-101215
    EvobrutinibInhibitor 98.17%
    Evobrutinib是 BTK 的抑制剂, 来自专利US20140162983 化合物实例0174。
  • HY-100342
    Ibrutinib-biotinInhibitor 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-100335
    PCI-33380Inhibitor 98.33%
    PCI-33380 是布鲁顿酪氨酸激酶 (BTK) 的不可逆抑制剂(荧光探针)。
  • HY-102036
    G-744Inhibitor
    G-744是有效,选择性的 Btk抑制剂,IC50 值为2 nM。
  • HY-101474
    (±)-ZanubrutinibInhibitor 99.70%
    (±)-Zanubrutinib 是一种有效的选择性 Bruton's 酪氨酸激酶 (Btk) 抑制剂。
  • HY-15771
    TirabrutinibInhibitor 99.31%
    Tirabrutinib (ONO-4059) 是高选择性,可口服的 BTK抑制剂,IC50 为2.2 nM。
  • HY-18012
    SpebrutinibInhibitor 99.95%
    Spebrutinib (AVL-292; CC-292) 是共价,高选择性和口服活性的 Btk抑制剂,IC50 为0.5 nM。
  • HY-101474A
    ZanubrutinibInhibitor 99.45%
    Zanubrutinib 是一个选择性的 Bruton tyrosine kinase(BTK) 抑制剂。
  • HY-15427
    GDC-0834Inhibitor 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-109078
    VecabrutinibInhibitor 99.96%
    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-80002
    BMX-IN-1Inhibitor 98.88%
    BMX-IN-1是BMX 激酶IC50 值为8.0 nM。
  • HY-101941
    BTK IN-1Inhibitor 98.88%
    BTK IN-1 是一种有效的 BTK抑制剂,IC50值<100 nM。
  • HY-112215
    ARQ 531Inhibitor 98.54%
    ARQ 531 是 BTK 可逆的非共价抑制剂,其对 WT-BTK 和 C481S-BTK 的 IC50 值分别为 0.85 nM 和 0.39 nM。
  • HY-18018
    RN486Inhibitor 99.38%
    RN486是高活性Btk抑制剂,IC50为4.0 nM。
  • HY-11999
    CGI-1746Inhibitor
    CGI-1746 是一种有效的,高选择性的 Btk抑制剂,IC50 值为 1.9 nM。
  • HY-112161
    BMS-986195Inhibitor 99.56%
    BMS-986195 是一个有效的、布鲁顿氏酪氨酸激酶 (BTK)的不可逆共价抑制剂,其IC50值<1 nM。
  • HY-112166
    PRN1008Inhibitor 99.49%
    PRN1008 是布鲁顿氏酪氨酸激酶 (BTK)可逆的、选择性的、有口服活性的共价抑制剂,其IC50 值为 1.3 nM。
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