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-176172
    BTK-IN-44
    		Inhibitor
    BTK-IN-44 (Compound 10) is a potent noncovalent inhibitor of Bruton’s tyrosine kinase (BTK) with an IC50 value of 24.7 nM. BTK-IN-44 interferes with signaling pathways of B cell malignancies, showing antitumor effects in lymphoma cells. BTK-IN-44 is promising for research of B cell malignancies (such as lymphoma).
    BTK-IN-44
  • HY-170413
    PROTAC BTK Degrader-12
    		Degrader
    PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based BTK degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: VHL ligand ( HY-W245311)).
    PROTAC BTK Degrader-12
  • HY-154860
    PTD10
    		Degrader
    PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834); Blue: E3 ligase ligand (HY-14658); Black: linker (HY-Y0966); E3 ligase ligand + linker (HY-131717)).
    PTD10
  • HY-158064
    BTK-IN-36
    		Inhibitor
    BTK-IN-36 (S-016) is a BTK inhibitor, with IC50 of 0.5 nM. BTK-IN-36 can be used in cancer-related research.
    BTK-IN-36
  • HY-144170
    RET-IN-14
    		Inhibitor
    RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
    RET-IN-14
  • HY-151961
    RSH-7
    		Inhibitor 99.07%
    RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.
    RSH-7
  • HY-150752
    BTK-IN-15
    		Inhibitor
    BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.
    BTK-IN-15
  • HY-175543
    BTK ligand 16
    		Ligand
    BTK ligand 16 is a BTK ligand that can be used for synthesis of TQ-3959 (HY-175541).
    BTK ligand 16
  • HY-123117
    VA5
    		Inhibitor
    VA5 is a BTK kinaseinhibitor. VA5 has the potential to be used to study diseases associated with BTK kinase activity.
    VA5
  • HY-159947
    PROTAC BTK Degrader-11
    		Degrader
    PROTAC BTK Degrader-11 is a PROTAC degrader that can break down BTK, with a DC50 of 1.7 nM. PROTAC BTK Degrader-11 can be used in cancer research. (Pink: target protein ligand (HY-159956); Black: linker; Blue: E3 ligase (HY-150839)).
    PROTAC BTK Degrader-11
  • HY-169307
    BTK-IN-38
    		Inhibitor
    BTK-IN-38 (Example 125) is a potent BTK inhibitor. BTK-IN-38 inhibits DOHH2 and BT474 cells proliferation with IC50s of 114 and 340 nM, respectively.
    BTK-IN-38
  • HY-175541
    TQ-3959
    		Degrader
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)).
    TQ-3959
  • HY-143720
    JAK3/BTK-IN-5
    		Inhibitor
    JAK3/BTK-IN-5 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, example 35)
    JAK3/BTK-IN-5
  • HY-148594
    BTK-IN-23
    		Inhibitor
    BTK-IN-23 is a BTK inhibitor (IC50: 12.8 nM). BTK-IN-23 also inhibits BLX and BMX with IC50s of 35.6 and 5.7 nM respectively. BTK-IN-23 shows improved kinase selectivity compared to Ibrutinib (HY-10997).
    BTK-IN-23
  • HY-172589
    BTK-IN-43
    		Inhibitor
    BTK-IN-43 (compound 9) is an inhibitor of BTK with an IC50 value of 21.6 nM. BTK-IN-43 has oral activity.
    BTK-IN-43
  • HY-147784
    HZ-A-005
    		Inhibitor
    HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models.
    HZ-A-005
  • HY-142932
    BTK-IN-6
    		Inhibitor
    BTK-IN-6 is a potent inhibitor of Bruton's Tyrosine Kinase (BTK). BTK is a member of the Tec family of tyrosine kinases and plays an important role in the regulation of early B-cell development and mature B-cell activation and survival. BTK-IN-6 has the potential for the research of immune disorders, cancer, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders, and neurological disorders (extracted from patent WO2021136219A1, compound 8).
    BTK-IN-6
  • HY-162081
    BTK-IN-32
    		Inhibitor
    BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain.
    BTK-IN-32
  • HY-150885
    BTK ligand 1
    		Degrader
    BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies.
    BTK ligand 1
  • HY-173126
    BTK ligand-14
    		Inhibitor
    BTK ligand-14 is a PROTAC target protein ligand that targets BTK and can be used for the synthesis of FDU73 (HY-173125).
    BTK ligand-14
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity