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-160167A
    (R,R)-Birelentinib
    		Inhibitor
    (R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies.
    (R,R)-Birelentinib
  • HY-176526
    BTK degrader-1 intermediate
    		Degrader
    BTK degrader-1 intermediate (compound 5) is an intermediate for the synthesis of BTK degrader-1 (HY-163295). BTK degrader-1 can be used as an ADC toxin to synthesize antibody-drug conjugate (ADC).
    BTK degrader-1 intermediate
  • HY-108691R
    PF-06465469 (Standard)
    		Inhibitor
    PF-06465469 (Standard) is the analytical standard of PF-06465469 (HY-108691). This product is intended for research and analytical applications. PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.
    PF-06465469 (Standard)
  • HY-101215R
    Evobrutinib (Standard)
    		Inhibitor
    Evobrutinib (Standard) is the analytical standard of Evobrutinib (HY-101215). This product is intended for research and analytical applications. 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 (Standard)
  • HY-135334S
    ACP-5862-d4
    		Inhibitor
    ACP-5862-d4 is deuterium labeled ACP-5862. 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-d<sub>4</sub>
  • HY-101766R
    Btk inhibitor 2 (Standard)
    		Inhibitor
    Btk inhibitor 2 (Standard) is the analytical standard of Btk inhibitor 2 (HY-101766). This product is intended for research and analytical applications. Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2 (Standard)
  • HY-101474BR
    (R)-Zanubrutinib (Standard)
    (R)-Zanubrutinib (Standard) is the analytical standard of (R)-Zanubrutinib (HY-101474B). This product is intended for research and analytical applications. (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 (Standard)
  • HY-128403
    BTK inhibitor 8
    		Inhibitor
    BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits Btk activity. BTK inhibitor 8 suppresses B cell activation. BTK inhibitor 8 is applicable to research related to arthritis and asthma.
    BTK inhibitor 8
  • HY-18012A
    Spebrutinib besylate
    		Inhibitor
    Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.
    Spebrutinib besylate
  • HY-101856R
    BMS-986142 (Standard)
    		Inhibitor
    BMS-986142 (Standard) is the analytical standard of BMS-986142 (HY-101856). This product is intended for research and analytical applications. 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 (Standard)
  • HY-18016
    CGI 560
    		Inhibitor
    CGI 560 is an inhibitor for Bruton's tyrosine kinase (BTK) with an IC50 of 400 nM.
    CGI 560
  • HY-10997AR
    Ibrutinib Racemate (Standard)
    		Inhibitor
    Ibrutinib (Racemate) (Standard) is the analytical standard of Ibrutinib (Racemate). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity