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-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-160966
    PROTAC BTK Degrader-10
    		Degrader
    PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader for BTK. PROTAC BTK Degrader-10 can be used for research of chronic lymphocytic leukemia (CLL)(Pink: ligand for target protein (HY-170758); Black: linker (HY-W392857); Blue: ligand for E3 ligase Cereblon (HY-W733176))
    PROTAC BTK Degrader-10
  • HY-147580
    BTK-IN-10
    		Inhibitor
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111).
    BTK-IN-10
  • HY-143717
    JAK3/BTK-IN-2
    		Inhibitor
    JAK3/BTK-IN-2 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-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)
    JAK3/BTK-IN-2
  • HY-124153
    GNE-431
    		Inhibitor
    GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases.
    GNE-431
  • HY-173143
    BTK-IN-42
    		Inhibitor
    BTK-IN-42 (Compound 11a) is a Btk inhibitor. BTK-IN-42 can effectively inhibit the growth and migration of tumor cells TMD8, with IC50 values of 2.61 and 5.34 μM for TMD8 and T9 cells respectively. It shows promise for research in the field of anti-cancer.
    BTK-IN-42
  • HY-139881
    BTK inhibitor 19
    		Inhibitor
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
    BTK inhibitor 19
  • HY-111781
    Civorebrutinib
    		Inhibitor
    Civorebrutinib (WS-413) is a Bruton's tyrosine kinase inhibitor with antineoplastic effect.
    Civorebrutinib
  • HY-157159
    BTK-IN-28
    		Inhibitor
    BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells.
    BTK-IN-28
  • HY-176131
    AMX5160
    		Inhibitor
    AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTKC481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases.
    AMX5160
  • HY-143900
    BTK-IN-7
    		Inhibitor
    BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity.
    BTK-IN-7
  • HY-156969
    Topoisomerase I inhibitor 11
    Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK.
    Topoisomerase I inhibitor 11
  • HY-117900A
    (Rac)-PF-06250112
    (Rac)-PF-0625011 is a racemate of PF-06250112. PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor and shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC.
    (Rac)-PF-06250112
  • HY-147741
    DPPY
    		Inhibitor
    DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
    DPPY
  • HY-145884
    BTK-IN-8
    		Inhibitor
    BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM).
    BTK-IN-8
  • 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: 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity