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-139481
    TL-895
    		Inhibitor 99.76%
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research.
    TL-895
  • HY-130983
    N-piperidine Ibrutinib hydrochloride
    		Inhibitor
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
    N-piperidine Ibrutinib hydrochloride
  • HY-109143
    Elsubrutinib
    		Inhibitor ≥98.0%
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
    Elsubrutinib
  • HY-18018
    RN486
    		Inhibitor 99.87%
    RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.
    RN486
  • HY-150023
    BI-1622
    		Inhibitor 98.97%
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
    BI-1622
  • HY-18951
    ONO-4059 analog
    		Inhibitor 99.74%
    ONO-4059 analog is an analogue of ONO-4059, and ONO-4059 (HY-15771) is a highly potent and selective Btk inhibitor.
    ONO-4059 analog
  • HY-15427A
    GDC-0834 Racemate
    		98.04%
    GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.
    GDC-0834 Racemate
  • HY-135334
    ACP-5862
    		Inhibitor 98.41%
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862
  • HY-15427B
    GDC-0834 (S-enantiomer)
    		98.03%
    GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834. GDC-0834 is a potent and selective BTK inhibitor.
    GDC-0834 (S-enantiomer)
  • HY-132879
    TAK-020
    		Inhibitor 99.93%
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
    TAK-020
  • HY-131342
    BIIB068
    		Inhibitor 99.69%
    BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
    BIIB068
  • HY-132842A
    (S)-Sunvozertinib
    		Inhibitor 99.14%
    (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
    (S)-Sunvozertinib
  • HY-101941
    BTK IN-1
    		Inhibitor 98.01%
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
    BTK IN-1
  • HY-101766
    Btk inhibitor 2
    		Inhibitor 99.57%
    Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2
  • HY-101856
    BMS-986142
    		Inhibitor 99.53%
    BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
    BMS-986142
  • HY-101474B
    (R)-Zanubrutinib
    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib (HY-101474A). (R)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 11 nM.
    (R)-Zanubrutinib
  • HY-136531
    XMU-MP-3
    		Inhibitor 98.27%
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
    XMU-MP-3
  • HY-153803
    GBD-9
    		Inhibitor 99.76%
    GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth.
    GBD-9
  • HY-153357
    NRX-0492
    		Degrader 98.16%
    NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex.
    NRX-0492
  • HY-153110A
    Larotinib mesylate hydrate
    		Inhibitor 98.66%
    Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
    Larotinib mesylate hydrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity