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-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-117628
    RN983
    		Inhibitor
    RN983 (Compound 1) is a highly selective Bruton's tyrosine kinase (Btk) inhibitor. RN983 inhibits IgG production in B-cells with an IC50 of 2.5 nM and PGD2 production from mast cells with an IC50 of 8.3 nM. RN983 is promising for research of asthma and other allergic diseases.
    RN983
  • HY-182943
    BTK-IN-49
    		Inhibitor
    BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC50 of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis.
    BTK-IN-49
  • HY-182671
    SRX3305
    		Inhibitor
    SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL.
    SRX3305
  • 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-180884
    BTK-IN-46
    		Inhibitor
    BTK-IN-46 (compound 24) is a reversible covalent BTK inhibitor. BTK-IN-46 covalently labels a lysine in the inositol phosphate (PIP3) binding site, thereby blocking Pleckstrin homology (PH) domain-mediated membrane recruitment and activation of BTK.
    BTK-IN-46
  • 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-182293
    BTK-IN-48
    		Inhibitor
    BTK-IN-48 is a BTK inhibitor with an IC50 of 1.14 μM. BTK-IN-48 inhibits recombinant BTK and c-Src, and exerts moderate inhibitory effects on LCK, BMX/ETK, FLT3 and PIM1. BTK-IN-48 can be used in the research of B-cell malignancies and autoimmune diseases.
    BTK-IN-48
  • 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-175788
    BTK ligand-17
    		Ligand
    BTK ligand-17 (The Target Protein Ligand Moiety of Catadegbrutinib) is a BTK ligand. BTK can be used as Ligands for Target Protein for PROTAC to develop and design degradative agents for PROTAC BTKs, such as Catadegbrutinib (HY-160141). BTK ligand-17 can also be used in cancer research.
    BTK ligand-17
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity