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-115944
    BTK-IN-9
    		Inhibitor
    BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells.
    BTK-IN-9
  • 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: CRBN 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-120406
    PLS-123
    		Inhibitor
    LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.
    PLS-123
  • 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-179562
    BTK degrader-2
    		Degrader
    BTK degrader-2 (Example 2) is a BTK dual-functional degrading agent, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases.
    BTK degrader-2
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity