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-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-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-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-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-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-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-139881
    BTK inhibitor 19
    		Inhibitor
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
    BTK inhibitor 19
  • 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-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
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