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-133137
    SJF620
    		Inhibitor 98.98%
    SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
    SJF620
  • HY-139481
    TL-895
    		Inhibitor 99.86%
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC50: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC50 = 1.6 nM) and TXK with IC50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC50: 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies.
    TL-895
  • 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-153357
    NRX-0492
    		Degrader 98.30%
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).
    NRX-0492
  • HY-P5438
    Srctide
    		Substrate 99.71%
    Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
    Srctide
  • HY-10997R
    Ibrutinib (Standard)
    		Inhibitor
    Ibrutinib (Standard) is the analytical standard of Ibrutinib. This product is intended for research and analytical applications. Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib (Standard)
  • HY-13943
    CNX-774
    		Inhibitor 99.92%
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.
    CNX-774
  • HY-19816A
    Avitinib maleate
    		Inhibitor 99.86%
    Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.
    Avitinib maleate
  • HY-107447
    N-Deshydroxyethyl Dasatinib
    		Ligand
    N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
    N-Deshydroxyethyl Dasatinib
  • HY-18009
    (Z)-LFM-A13
    		Inhibitor 99.80%
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
    (Z)-LFM-A13
  • HY-78727
    Ibrutinib deacryloylpiperidine
    		Inhibitor 99.96%
    Ibrutinib deacryloylpiperidine (IBT4A) is a derivative of an Ibrutinib (HY-10997) intermediate and an Ibrutinib impurity. Ibrutinib deacryloylpiperidine serves as a starting material and is used in the synthesis of a modified BTK inhibitor derivative via the Mitsunobu reaction.
    Ibrutinib deacryloylpiperidine
  • HY-163962
    L18I
    		99.89%
    L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964)[1].
    L18I
  • HY-101474
    (±)-Zanubrutinib
    		Inhibitor 99.70%
    (±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 0.63 nM.
    (±)-Zanubrutinib
  • HY-15427
    GDC-0834
    		Inhibitor 98.05%
    GDC-0834 is an orally active selective, potent, and reversible BTK inhibitor with an IC50 of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA).
    GDC-0834
  • HY-122830
    DD-03-171
    		Degrader 98.72%
    DD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC50 = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)).
    DD-03-171
  • HY-163295
    BTK degrader-1
    		Degrader 99.40%
    BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect.
    BTK degrader-1
  • HY-144288
    BLK-IN-2
    		Inhibitor 98.61%
    BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC50 of 5.9 nM. BLK-IN-2 also inhibits BTK (IC50=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells.
    BLK-IN-2
  • HY-100338
    CNX-500
    		Inhibitor 99.86%
    CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
    CNX-500
  • HY-49421
    BTK ligand 12
    		Ligand 98.23%
    BTK ligand 12 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BTK ligand 12 can serve as an active control for the target protein ligand of NRX-0492 (HY-153357).
    BTK ligand 12
  • HY-101856
    BMS-986142
    		Inhibitor 99.38%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity