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-171131
    BTK-IN-41
    		Inhibitor
    BTK-IN-41 (Compound 47) is the inhibitor for BTK with an IC50 of 5.4 nM. BTK-IN-41 inhibits the diffuse large B cell lymphoma cell TDM-8 with IC50 of 13.8 nM.
    BTK-IN-41
  • HY-160219S
    BTK-IN-33
    		Inhibitor
    BTK-IN-33 is a Btk inhibitor with anticancer effects (WO2023174300A1; compound I).
    BTK-IN-33
  • HY-164002
    PF-303
    		Inhibitor
    PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation.
    PF-303
  • HY-170324
    BTK-IN-40
    		Inhibitor
    BTK-IN-40 (compound 375) is a BTK inhibitor.
    BTK-IN-40
  • HY-169228
    WS-11
    		Inhibitor
    WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds.
    WS-11
  • HY-182933
    BTK ligand-20
    		Ligand
    BTK ligand-20 (compound 1) is a BTK ligand. BTK ligand-20 serves as a target protein ligand for the synthesis of PROTAC BTK Degrader-15 (HY-182910). BTK ligand-20 is applicable to cancer research.
    BTK ligand-20
  • HY-156745
    DDa-1
    		Degrader
    DDa-1 is a potent BTK degrader (DC50: 90 nM). Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BTK ligand (HY-107447).
    DDa-1
  • HY-171893
    CRBN ligand-185
    		Ligand
    CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948 (HY-153321).
    CRBN ligand-185
  • HY-155072
    PROTAC BTK Degrader-5
    		Degrader
    PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898))1.
    PROTAC BTK Degrader-5
  • HY-153951S
    BTK-IN-26
    		Inhibitor
    BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research.
    BTK-IN-26
  • HY-160168
    BTK-IN-31
    		Inhibitor
    BTK-IN-31 (Compound 2) is a selective, non-covalently reversible, and blood-brain barrier (BBB) permeable Btk inhibitor. BTK-IN-31 has research potential in immune disorders, cancer, cardiovascular disease, viral infections, inflammation, metabolic/endocrine dysfunction, and neurological disorders.
    BTK-IN-31
  • HY-162407
    I-As-1
    		Inhibitor
    I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC50 of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC50s of 0.52 μM and 0.11 μM, respectively.
    I-As-1
  • HY-162257
    BTK-IN-34
    		Inhibitor
    BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway.
    BTK-IN-34
  • HY-160167
    Birelentinib
    		Inhibitor
    Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL).
    Birelentinib
  • HY-151920
    BTK-IN-17
    		Inhibitor
    BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects.
    BTK-IN-17
  • HY-144283
    BLK-IN-1
    		Inhibitor
    BLK-IN-1 (compound 1) is a selective and covalent inhibitor of B-Lymphoid tyrosine kinase (BLK) and BTK, with IC50s of 18.8 nM and 20.5 nM, respectively. BLK-IN-1 can be used for the research of cancer.
    BLK-IN-1
  • HY-142621
    BCPyr
    		Inhibitor
    BCPyr is a PROTAC-class BTK degrader (DC50 = 800 nM). BCPyr consists of a PROTAC target protein ligand (red part) BTK ligand 11 (HY-168314), an E3 ubiquitin ligase ligand (blue part) E3 ligase Ligand 20 (HY-135997), and a PROTAC linker (black part) (5-(Bromomethyl)pyrazin-2-yl)methanol (HY-168315). E3 ubiquitin ligase+linker can form E3 Ligase Ligand-linker Conjugate 146 (HY-168316).
    BCPyr
  • HY-P10609
    Btk substrate peptide
    Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases.
    Btk substrate peptide
  • HY-181546
    Ibt-DOX
    		Inhibitor
    Ibt-DOX is a BTK inhibitor with an IC50 of 2.89 nM. Ibt-DOX is also a targeted covalent activated chemotherapeutic agent composed of the targeting ligand Ibrutinib (HY-10997), Doxorubicin (DOX) (HY-15142A), α-MAA (HY-W017180), and a linker (HY-Y0892). Ibt-DOX specifically binds to BTK and releases DOX, synergistically achieving BTK inhibition and chemotherapeutic killing, significantly enhancing toxicity against B-cell lymphoma cells and greatly reducing the toxic side effects of DOX on BTK-negative cells. Ibt-DOX can be used in lymphoma-related research.
    Ibt-DOX
  • HY-181547
    HBC-12551
    		Inhibitor
    HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTKC481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma.
    HBC-12551
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity